1-1-diphenyl-2-picrylhydrazyl and Disease-Models--Animal

It is recognized that the properties of liquid water can be markedly different from those of bulk one when it is in contact with hydrophobic surfaces or is confined in nano-environments. Because our knowledge regarding water structure on the molecular level of dynamic equilibrium within a picosecond time scale is far from completeness all of water's conventionally known properties are based on inert "bulk liquid water" with a tetrahedral hydrogen-bonded structure. Actually, the strength of water's hydrogen bonds (HBs) decides its properties and activities. In this review, an innovative idea on preparation of metastable plasmon-activated water (PAW) with intrinsically reduced HBs, by letting deionized (DI) water flow through gold-supported nanoparticles (AuNPs) under resonant illumination at room temperature, is reported. Compared to DI water, the created stable PAW can scavenge free hydroxyl and 2,2-diphenyl-1-picrylhydrazyl radicals and effectively reduce NO release from lipopolysaccharide-induced inflammatory cells. Moreover, PAW can dramatically induce a major antioxidative

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Disease Models, Animal; Fibroblasts; Gene Expression; Gold; Humans; Hydrogen Bonding; Lipopolysaccharides; Lung Neoplasms; Nanoparticles; NF-E2-Related Factor 2; Nitric Oxide; Picrates; Renal Insufficiency, Chronic; Sleep Deprivation; Surface Plasmon Resonance; Water

Humans rely on plants as a necessitous source of their food, energy, cosmetics and medicines, as medicinal plants are rich source of new therapeutically active compounds from decades. Current study was designed to separate and identify active constituents of Erythrina suberosa bark extract using phytochemical screening and gas chromatography and mass spectroscopy, respectively and evaluated their therapeutic activities. E. suberosa bark extract contained saponins, glycosides, alkaloids, tannins, terpenoids, phenols and 44 active compounds identified by phytochemical and gas chromatography and mass spectroscopic analysis. Therapeutic potentials of E. suberosa bark extract was evaluated by such as cytotoxicity, anti-inflammatory and antioxidant assay. Surprisingly, bark extract shows the concentration dependent cytotoxicity against human fibroblast malignant melanoma-144 cell lines and remarkably inhibited (15.18(plusmn;1.13%, at 400mg/ml) growth of cancer cells after 24 hours treatment. In addition, the E. suberosa bark extract also exhibited anti-inflammatory effect at higher doses (400mg/kg) and moderate antioxidant activity is also noticed through (2, 2-diphenyl-1-picrylhydrazyl radical) assay. These findings indicate that E. suberosa bark extract exhibited prominent anticancer and anti-inflammatory activities and might be serve as a potent therapeutic agent in future.

Topics: Animals; Anti-Inflammatory Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Biphenyl Compounds; Carrageenan; Cell Line, Tumor; Cell Proliferation; Chemical Fractionation; Disease Models, Animal; Erythrina; Gas Chromatography-Mass Spectrometry; Humans; Inflammation; Neoplasms; Phytochemicals; Picrates; Plant Bark; Plant Extracts; Rats

Colocasia gigantea, locally named as kochu is well-known due to its various healing power. This research is to investigate the antidiarrheal, antimicrobial and antioxidant possibilities of the methanol soluble extract of Colocasia gigantea.. The antidiarrheal investigation was performed by using in vivo castor oil-induced diarrheal method whereas in vitro antimicrobial and antioxidant investigation have been implemented by disc diffusion and DPPH scavenging method respectively. Moreover, in silico studies were followed by molecular docking analysis of several secondary metabolites that were appraised with Schrödinger-Maestro v11.1 and Biovia Discovery Studio.. The induction of plant extract (200 and 400 mg/kg, b.w, p.o) has minimized the castor oil mediated diarrhea by 16.96% (p < 0.01) and 38.89% (p < 0.001) respectively compared to control group. The methanol extract of C. gigantea showed mild sensitivity against almost all the tested strains but it shows high consistency of phenolic content and yielded 67.68 μg/mL of IC. The results of this scientific research reflects that the methanol soluble extract of C. gigantea is safe and may provide possibilities of alleviation of diarrhea along with being a potential wellspring of antioxidant and antimicrobial agents which can be considered as an alternate source for exploration of new medicinal products in near future.

Topics: Animals; Anti-Bacterial Agents; Antidiarrheals; Antioxidants; Biphenyl Compounds; Colocasia; Disease Models, Animal; Escherichia coli; Female; Inhibitory Concentration 50; Male; Mice; Molecular Docking Simulation; Phytotherapy; Picrates; Plant Extracts; Plant Leaves

Red yeast rice (RYRP) has been utilized for coloring food, brewing wine, and preserving meat, which is also used as a folk medicine for centuries. In this study, a water-soluble nonstarch polysaccharide from RYRP was extracted by using ultrasonic-assisted extraction method. By using the Box-Behnken design to optimize the parameters for extracting the RYRP, the maximum extraction yield (3.37 ± 0.78%) was obtained under the optimal extraction conditions as follows: ratio of water to raw material (40 mL/g), extraction temperature (62 °C), extraction time (75 Min), and ultrasonic power (200 W). Moreover, monosaccharide composition analysis showed that RYRP was consisted of mannose, glucosamine, glucose, and galactose with a molar ratio of 0.152:0.015:1:0.149. The molecular weight distribution analysis showed that the average molecular weight of the RYRP fraction was about 3.49 × 10

Topics: Administration, Oral; Animals; Antioxidants; Biological Products; Biphenyl Compounds; Carbohydrate Conformation; Disease Models, Animal; Dose-Response Relationship, Drug; Female; Gastrointestinal Diseases; Male; Mice; Mice, Inbred Strains; Molecular Weight; Particle Size; Picrates; Polysaccharides; Surface Properties; Temperature; Time Factors; Ultrasonic Waves

Heliangolide is a naturally occurring sesquiterpene lactone and its derivatives are biologically active compounds present in most medicinal plants. This study evaluated the antioxidant and antidiabetic properties of a heliangolide sesquiterpene lactone isolated from Helianthus annuus L. leaves. The heliangolide sesquiterpene lactone was isolated through a combination of solvent-solvent partitioning, column chromatography, thin layer chromatography and high-performance liquid chromatography techniques. The antioxidant activity of the compound was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide radical scavenging assays while the antidiabetic effects were investigated in alloxan-induced diabetic rats. The heliangolide derivative at the concentration of 954.2 µmol L-1 showed 23.7 % DPPH and 26 % nitric oxide radical inhibitions compared with 96.6 and 50.9 %, resp., displayed by the controls (2,271.2 µmol L-1). It also reduced the fasting blood glucose (FBG) levels in a time-dependent manner. The highest activity was recorded within 6 h post-treatment at 0.2 mmol kg-1 bm. The heliangolide derivative exhibited significant (p < 0.05) antioxidant and antidiabetic properties and provides a basis for further development of constituents of Helianthus annuus leaves for the management of such diseases.

Topics: Animals; Antioxidants; Biphenyl Compounds; Diabetes Mellitus, Experimental; Disease Models, Animal; Flavonoids; Helianthus; Hypoglycemic Agents; Lactones; Male; Picrates; Plant Extracts; Plant Leaves; Plants, Medicinal; Rats; Rats, Wistar; Sesquiterpenes

Necrotizing enterocolitis (NEC) is the most common life-threatening gastrointestinal disease encountered in the premature infant. It has been shown that the intercellular reactive oxygen species (ROS) generation activated by lipopolysaccharide involved in the nuclear factor kappa B (NF-κB) activation and pathogenesis of NEC. Here, we report that an antioxidant peptide from tuna backbone protein (APTBP) reduces the inflammatory cytokines transcription and release. APTBP directly scavenges the free radical through 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2-phenyl-4,4,5,5-tetramethylimidazoline-1-oxyl 3-oxide (PTIO) assay. In addition, APTBP reduces the intracellular ROS level, exhibiting an antioxidant activity within cells. Remarkably, gavage with APTBP attenuates the phenotype of NEC in the mice model. Mechanically, the NF-κB activation, together with the expression of inflammatory cytokines are decreased significantly when intracellular ROS are eliminated by APTBP. Therefore, our findings demonstrated that an antioxidant peptide, APTBP, ameliorates inflammation in NEC through attenuating ROS-NF-κB axis.

Topics: Animals; Animals, Newborn; Biphenyl Compounds; Cyclic N-Oxides; Cytokines; Disease Models, Animal; Enterocolitis, Necrotizing; Humans; Imidazoles; Inflammation; Intestinal Mucosa; Lipopolysaccharides; Mice; NF-kappa B; Peptides; Picrates; Rats; Reactive Oxygen Species; Tuna

A new series of 2-(4-acetyl-3-methyl-5-(arylamino) thiophen-2- yl)-3-arylquinazolin-4(3H)-one derivatives (11a-11j) were synthesized from acetyl acetone, phenyl isothiocyanate and 2-chloromethyl quinazolinone.. Due to side effects of Non Steroidal Anti-Inflammatory Drugs (NSAID), an attempt was made to identify the novel tetrasubstituted thiophene lead compound as potential anti-inflammatory and antioxidant agent.. Then newly synthesized compounds were characterized by IR spectroscopy, 1H NMR and mass spectrometry. The synthesized compounds were screened for their in vivo anti-inflammatory activity in carrageenan-induced rat hind paw edema model at dose 20mg/kg body weight using diclofenac sodium as a standard drug. The compounds were also evaluated for their in vitro DPPH free radical-scavenging activity and nitric oxide radical scavenging activity at the concentrations of 10, 20, 40, 60, 80 and 100 µg/mL using ascorbic acid as standard drug.. The results from carrageenan-induced rat hind paw edema showed that compounds 11e, 11f and 11b show a significant anti-inflammatory activity of 46.61%, 48.94% and 47.04 % protection respectively to inflamed paw but less than diclofenac sodium. Compounds 11h and 11e show good DPPH free radical scavenging and nitric oxide radical scavenging activity, respectively.. From results, it was observed that highly substituted thiophene scaffold exhibits anti-inflammatory and antioxidant activity.

Topics: Animals; Anti-Inflammatory Agents; Biphenyl Compounds; Carrageenan; Diclofenac; Disease Models, Animal; Dose-Response Relationship, Drug; Edema; Free Radical Scavengers; Male; Mice; Molecular Structure; Nitric Oxide; Picrates; Quinazolines; Rats, Wistar; Structure-Activity Relationship; Thiophenes

To find bioactive medicinal herbs exerting anti-asthmatic activity, we investigated the effect of an aqueous extract of Urtica dioica L. (Urticaceae) leaves (UD), the closest extract to the Algerian traditional use.. In this study, we investigated the in vivo anti-asthmatic and antioxidant activities of nettle extract.. Adult male Wistar rats were divided into four groups: Group I: negative control; group II: Ovalbumin sensitized/challenged rats (positive control); group III: received UD extract (1.5 g/kg/day) orally along the experimental protocol; group IV: received UD extract (1.5 g/kg/day) orally along the experimental protocol and sensitized/challenged with ovalbumin. After 25 days, blood and tissue samples were collected for haematological and histopathological analysis, respectively. The oxidative stress parameters were evaluated in the lungs, liver and erythrocytes. Then, correlations between markers of airway inflammation and markers of oxidative stress were explored.. UD extract significantly (p < 0.01) inhibited eosinophilia increases in BALF (-60%) and the levels of leucocytes (-32.75%) and lymphocytes (-29.22%) in serum, and effectively suppressed inflammatory cells recruitment in the asthmatic rat model. Besides, the lipid peroxidation generated by allergen administration was significantly (p < 0.05) diminished by UD treatment in lung tissue (-48.58%). The nettle extract was also investigated for the total phenolic content (30.79 ± 0.96 mg gallic acid/g dry extract) and shows DPPH radical scavenging activity with 152.34 ± 0.37 μg/mL IC. The results confirmed that UD administration might be responsible for the protective effects of this extract against airway inflammation.

Topics: Animals; Anti-Asthmatic Agents; Anti-Inflammatory Agents; Antioxidants; Asthma; Biphenyl Compounds; Disease Models, Animal; Lipid Peroxidation; Lung; Male; Ovalbumin; Oxidative Stress; Phenols; Phytotherapy; Picrates; Plant Extracts; Plant Leaves; Plants, Medicinal; Pneumonia; Pulmonary Eosinophilia; Rats, Wistar; Urtica dioica

We investigated the effect of the culinary-medicinal mushroom Pleurotus eryngii var. ferulae DDL01 on oxidative damage in the liver and brain and a high-fat/high-cholesterol-induced hyperlipidemic model. In in vitro studies, the water extracts of the fruiting bodies showed strong scavenging activities of DPPH (139.46 ± 3.2 μg) and hydroxyl (139.46 ± 3.2 μg) radicals. Moreover, the extracts showed Fe2+ chelating and reducing abilities, as well as a large amount of polyphenols and an inhibitory effect on lipid peroxidation in the liver and brain tissues. The rats were fed a pellet diet (7.5 g/rat/day) containing P. eryngii var. ferulae DDL01 (PD) for 3 weeks. In the high-fat/high-cholesterol-induced hyperlipidemic rat model, administration of PD caused a significant decrease (P < 0.05) in the levels of serum triacylglycerols, low-density lipoprotein cholesterol, very-low-density lipoprotein cholesterol, aspartate aminotransferase, and alanine aminotransferase and a significant increase (P < 0.05) in the level of high-density lipoprotein cholesterol. PD administration significantly decreased high-fat/high-cholesterol-induced hepatic lipid accumulation. Treatment with the extracts (up to 500 μg/mL) did not significantly affect the viability of HepG2 and 3T3-L1 cells. Our findings suggest that this mushroom has potential as an antiatherogenic dietary source in the development of therapeutic agents and functional foods.

Topics: Agaricales; Alanine Transaminase; Animals; Antioxidants; Aspartate Aminotransferases; Biphenyl Compounds; Cell Line; Cell Survival; Diet, High-Fat; Disease Models, Animal; Fatty Liver; Hepatocytes; Humans; Hydroxyl Radical; Hyperlipidemias; Hypolipidemic Agents; Lipoproteins; Picrates; Pleurotus; Rats; Treatment Outcome; Triglycerides

Mushrooms are valued for their nutritional as well as medicinal properties. Ganoderma species are used traditionally to treat neurological disorders but scientific evidence for this is insufficient. The present study was designed to systematically evaluate the anti-amnesic effect of selected Ganoderma species i.e. G. mediosinense and G. ramosissimum. Extracts of selected mushroom species were evaluated for their antioxidant activity and acetylcholinesterase (AChE) inhibition using in-vitro assays (DPPH and Ellman tests respectively). The anti-amnesic potential of the most active extract (i.e. 70% methanol extract of G. mediosinense) was confirmed using mouse model of scopolamine-induced amnesia. Mice were treated with bioactive extract and donepezil once orally before the induction of amnesia. Cognitive functions were evaluated using passive shock avoidance (PSA) and novel object recognition (NOR) tests. The effect on brain AChE activity, brain oxidative stress (TBARS level) and neuronal damage (H & E staining) were also assessed. In-vitro results showed strong antioxidant and AChE inhibitory activities by G. mediosinense extract (GME). Therefore, it was selected for in-vivo studies. GME pre-treatment (800mg/kg, p.o.) reversed the effect of scopolamine in mice, evident by significant decrease (p <0.05) in the transfer latency time and increase in object recognition index in PSA and NOR, respectively. GME significantly reduced the brain AChE activity and oxidative stress. Histopathological examination of brain tissues showed decrease in vacuolated cytoplasm and increase in pyramidal cells in brain hippocampal and cortical regions. GME exerts anti-amnesic effect through AChE inhibition and antioxidant mechanisms.

Topics: Acetylcholinesterase; Amnesia; Animals; Antioxidants; Avoidance Learning; Behavior, Animal; Biphenyl Compounds; Brain; Cholinesterase Inhibitors; Cognition; Disease Models, Animal; Donepezil; Dose-Response Relationship, Drug; Ganoderma; GPI-Linked Proteins; Indans; Male; Memory; Mice; Nootropic Agents; Picrates; Piperidines; Reaction Time; Recognition, Psychology; Scopolamine; Time Factors

Currently, there has been an increased interest globally to identify natural compounds that are pharmacologically potent and have low or no adverse effects for use in preventive medicine. Myocardial infarction is a vital pathological feature resulting in high levels of mortality and morbidity. Left ventricular hypertrophy (LVH), adenosine triphosphatases (ATPases) dysfunction and electrolyte imbalance play a vital role in the pathogenesis of myocardial infarction. This study aims to evaluate the preventive effects of diosmin on LVH, ATPases dysfunction and electrolyte imbalance in isoproterenol induced myocardial infarcted rats. Male albino Wistar rats were pretreated orally with diosmin (10mg/kg body weight) daily for a period of 10 days. After pretreatment, isoproterenol (100mg/kg body weight) was injected subcutaneously into the rats twice at an interval of 24h to induce myocardial infarction. Isoproterenol induced myocardial infarcted rats showed increased LVH, altered levels/ concentrations of serum cardiac troponin-T, heart ATPases, heart sodium ion, calcium ion and potassium ion, and increased myocardial infarct size. Pretreatment with diosmin revealed preventive effects on LVH, and all the above mentioned biochemical parameters evaluated in isoproterenol induced myocardial infarcted rats. The 2, 3, 5-triphenyl tetrazolium chloride staining on myocardial infarct size confirmed the prevention of myocardial infarction. Further, the 1, 1 diphenyl-2- picryl-hydrazyl (DPPH) radical in vitro study revealed a potent DPPH free radical scavenging action of diosmin. Thus, the observed effects of diosmin are due to its antihypertrophic and free radical scavenging activities in isoproterenol induced myocardial infarcted rats.

Topics: Adenosine Triphosphatases; Animals; Biphenyl Compounds; Diosmin; Disease Models, Animal; Electrolytes; Hypertrophy, Left Ventricular; Male; Myocardial Infarction; Picrates; Rats; Rats, Wistar

The defatted seeds of Camellia oleifera var. monosperma Hung T. Chang (Theaceae) are currently discarded without effective utilization. However, sapogenin has been isolated and shows antioxidative, anti-inflammatory and analgesic activities suggestive of its neuroprotective function.. In order to improve the activities of sapogenin, the nanoparticles of iron-sapogenin have been synthesized, and the neuroprotective effects are evaluated.. Structural characters of the nanoparticles were analyzed, and the antioxidant effect was assessed by DPPH method, and the neuroprotective effect was evaluated by rotenone-induced neurodegeneration in Kunming mice injected subcutaneously into the back of neck with rotenone (50 mg/kg/day) for 6 weeks and then treated by tail intravenous injection with the iron-sapogenin at the dose of 25, 50 and 100 mg/kg for 7 days. Mice behaviour and neurotransmitters were tested.. The product had an average size of 162 nm with spherical shape, and scavenged more than 90% DPPH radicals at 0.8 mg/mL concentration. It decreased behavioural disorder and malondialdehyde content in mice brain, and increased superoxide dismutase activity, tyrosine hydroxylase expression, dopamine and acetylcholine levels in brain in dose dependence, and their maximum changes were respectively up to 60.83%, 25.17%, 22.13%, 105.26%, 42.17% and 22.89% as compared to vehicle group. Iron-sapogenin nanoparticle shows significantly better effects than the sapogenin.. Iron-sapogenin alleviates neurodegeneration of mice injured by neurotoxicity of rotenone, it is a superior candidate of drugs for neuroprotection.

Topics: Acetylcholine; Animals; Behavior, Animal; Biomarkers; Biphenyl Compounds; Brain; Camellia; Chlorides; Disease Models, Animal; Dopamine; Dose-Response Relationship, Drug; Drug Compounding; Ferric Compounds; Free Radical Scavengers; Injections, Intravenous; Injections, Subcutaneous; Male; Malondialdehyde; Metal Nanoparticles; Mice; Motor Activity; Nerve Degeneration; Neuroprotective Agents; Oxidative Stress; Phytotherapy; Picrates; Plants, Medicinal; Rotenone; Sapogenins; Seeds; Superoxide Dismutase; Tyrosine 3-Monooxygenase

Bryophyllum pinnatum (Lam.) Kurz (Crassulaceae) is a plant known for its antiulcer properties.. This study evaluates the anti-Helicobacter pylori activity of Bryophyllum pinnutum methanol extract with a mouse model and its antioxidant properties.. Dried leaves of Bryophyllum pinnutum were extracted with methanol and ethyl acetate. Broth microdilution method was used to evaluate the anti-Helicobacter activity of extract samples in vitro. Swiss mice were inoculated with a suspension of Helicobacter pylori and divided into control group and four others that received 125, 250, 500 mg/kg of methanol extract or ciprofloxacin (500 mg/kg), respectively, for 7 days. Helicobacter pylori colonization and bacterial load of mouse stomach was assessed on day 1 and 7 post-treatment. The antioxidant activity of Bryophyllum pinnutum was evaluated through DPPH radical, hydroxyl radical and reducing power assay.. The data suggest that the methanol extract of Bryophyllum pinnatum could inhibit Helicobacter pylori growth, and may also acts as an antioxidant to protect gastric mucosa against reactive oxygen species.

Topics: Animals; Anti-Bacterial Agents; Antioxidants; Bacterial Load; Biphenyl Compounds; Disease Models, Animal; Gastric Mucosa; Helicobacter Infections; Helicobacter pylori; Hydroxyl Radical; Kalanchoe; Methanol; Mice; Microbial Sensitivity Tests; Oxidation-Reduction; Phytotherapy; Picrates; Plant Extracts; Plant Leaves; Plants, Medicinal; Solvents; Time Factors

To date, spinal cord injury (SCI) has remained an incurable disaster. The use of self-assembling peptide nanofiber containing bioactive motifs such as bone marrow homing peptide (BMHP1) as an injectable scaffold in spinal cord regeneration has been suggested. Human endometrial-derived stromal cells (hEnSCs) have been approved by the FDA for clinical application. In this regard, we were interested in investigating the role of BMHP1 in hEnSCs' neural differentiation in vitro and evaluating the supportive effects of this scaffold in rat model of chronic SCI. 1,1-Diphenyl-2-picryl-hydrazyl (DPPH), lactate dehydrogenase (LDH) release, 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) assay, real-time PCR, and immunocyotochemistry (ICC) were performed as a biocompatibility and neural differentiation evaluations on neuron-like hEnSC-derived cells encapsulated into nanofiber. Nanofiber was implanted into rats and followed by behavioral test, Nissl, luxol fast blue (LFB) staining and immunohistostaining (IHC). Results indicated that cell membrane of neuroblastoma cells were more sensitive than hEnSCs to concentration of proton and cell proliferation decreased with increase of concentration. This effect might be related to oxygen tension and elastic modules of scaffold. -BMHP1 nanofiber induced neural differentiation in hEnSC and decreased GFAP gene and protein as a marker of reactive astrocytes in vitro and in vivo. A reason for this finding might be related to the role of spacer number in induction of mechano-transduction signals. The presented study revealed the chimeric BMHP1 nanofiber induced higher axon regeneration and myelniation around the cavity and motor neuron function was encouraged to improve with less inflammatory response following SCI in rats. These effects were possibly due to nanostructured topography and mechano-transduction signals derived from hydrogel at low concentration.

Topics: Acyltransferases; Adult; Amino Acid Motifs; Animals; Biomarkers; Biphenyl Compounds; Blood-Brain Barrier; Cell Line, Tumor; Cell Survival; Chromatography, High Pressure Liquid; Chromatography, Reverse-Phase; Chronic Disease; Disease Models, Animal; Endometrium; Female; Humans; L-Lactate Dehydrogenase; Male; Motor Neurons; Nanofibers; Picrates; Rats, Wistar; Real-Time Polymerase Chain Reaction; Recovery of Function; Spinal Cord Injuries; Stromal Cells

Cajanus cajan L. (Fabaceae), a food crop, is widely used in traditional medicine.. The phytochemical composition of C. cajan seeds and evaluation of the anti-inflammatory, immunomodulatory, antinociceptive, and antioxidant activities were studied.. Unsaponifiable matter and fatty acids were analyzed by GC and GC/MS. The n-butanol fraction was chromatographed on polyamide column. The anti-inflammatory activity of hexane extract (200 and 400 mg/kg, p.o.) was evaluated using the carrageenan-induced rat paw edema at 1, 2, and 3 h. The serum tumor necrosis factor-α, interleukin-6, and immunoglobulin G levels were detected by ELISA. The hexane extract antinociceptive activity was determined by adopting the writhing test in mice. DPPH radical scavenging, total reduction capability, and inhibition of lipid peroxidation of butanol fraction were evaluated.. Twenty-one unsaponifiable compounds (mainly phytol, 2,6-di-(t-butyl)-4-hydroxy-4-methyl-2,5-cyclohexadiene-1-one, β-sitosterol, stigmasterol, and campesterol), as well as 12 fatty acids (primarily 9,12-octadecadienoic and palmitic acids) were identified in hexane extract of C. cajan seeds. n-BuOH fraction contains quercetin-3-O-β-d-glucopyranoside, orientin, vitexin, quercetin, luteolin, apigenin, and isorhamnetin. For the first time, quercetin-3-O-β-d-glucopyranoside is isolated from C. cajan plant. The hexane extract (200 and 400 mg/kg) inhibited carrageenan-induced inflammation by 85 and 95%, respectively, 3 h post-carrageenan challenge. This was accompanied by an 11 and 20%, 8 and 13%, respectively, decrease of TNF-α and IL-6, as well as significant decrease in IgG serum levels. Moreover, hexane extract (200 and 400 mg/kg) decreased the number of writhings by 61 and 83%, respectively. The butanol fraction showed DPPH radical scavenging (inhibitory concentration (IC50) value: 9.07 μg/ml).

Topics: Analgesics; Animals; Anti-Inflammatory Agents; Antioxidants; Behavior, Animal; Biphenyl Compounds; Butanols; Cajanus; Carrageenan; Cytokines; Disease Models, Animal; Egypt; Female; Gas Chromatography-Mass Spectrometry; Hexanes; Immunologic Factors; Inflammation; Inflammation Mediators; Lipid Peroxidation; Male; Mice; Nociceptive Pain; Phytotherapy; Picrates; Plant Extracts; Plants, Medicinal; Rats; Seeds; Solvents; Time Factors

Context Hamelia patens Jacq. (Rubiaceae) is traditionally used to treat wounds, inflammation and diabetes. However, there is still a lack of scientific evidence to support these applications. Objective The objective of this study is to evaluate the anti-inflammatory, antioxidant and antidiabetic activities of Hamelia patens, and identify its bioactive compounds. Materials and methods Four extracts were obtained by maceration and liquid-liquid extraction: HEX, DCM-EtOAc, MeOH-EtOAc and MeOH-Aq. The anti-inflammatory effect was evaluated orally on rat paw carrageenan-induced oedema over 6 h (50, 200 and 500 mg/kg), and topically in mouse ear oedema induced by 12-tetradecanoylphorbol-13-acetate (TPA) after 4 h (0.5 and 1 mg/ear). We also evaluated myeloperoxidase levels in ear tissue, 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging ability, and in vitro α-glucosidase inhibition. The chemical compounds were separated by column chromatography and identified by spectroscopic analysis. Results We found that the oral administration of the HEX extract at 500 and 200 mg/kg significantly decreased the carrageenan-induced inflammation after 1 and 3 h, respectively. The MeOH-EtOAc extract significantly inhibited myeloperoxidase activity (83.5%), followed by the DCM-EtOAc extract (76%), β-sitosterol/stigmasterol (72.7%) and the HEX extract (55%), which significantly decreased oedema induced by TPA at both doses, giving a similar effect to indomethacin. We also found that the MeOH-EtOAc, MeOH-Aq and DCM-EtOAc extracts showed good DPPH scavenging activity (IC50 values of 18.6, 93.9 and 158.2 μg/mL, respectively). The HEX extract showed the lowest α-glucosidase inhibition (an IC50 value of 26.07 μg/mL), followed by the MeOH-EtOAc extract (an IC50 value of 30.18 μg/mL), β-sitosterol/stigmasterol (IC50 34.6 μg/mL) and compound A ((6E,10E,14E,18E)-2,6,10,14,18,23-hexamethyl-2,6,10,14,18,22-tetracosahexaene, an IC50 value of 114.6 μg/mL), which were isolated for the first time from Hamelia patens. Discussion and conclusion Hamelia patens possesses anti-inflammatory, antioxidant and α-glucosidase inhibitory activities, which support its traditional use. These effects can be attributed to the identified compounds.

Topics: alpha-Glucosidases; Animals; Anti-Inflammatory Agents; Biphenyl Compounds; Carrageenan; Disease Models, Animal; Dose-Response Relationship, Drug; Edema; Female; Free Radical Scavengers; Glycoside Hydrolase Inhibitors; Hamelia; Peroxidase; Phytotherapy; Picrates; Plant Leaves; Plants, Medicinal; Rats, Wistar; Saccharomyces cerevisiae Proteins; Solvents; Tetradecanoylphorbol Acetate; Time Factors

Context Ligularia fischeri (Ledebour) Turcz. (Compositae) has been used as a leafy vegetable and in traditional medicine to treat hepatic disorder in East Asia. Objective The present study explores the antioxidant activity of LF aqueous extract on EtOH-induced oxidative stress accompanied by hepatotoxicity both in vitro and in vivo. Materials and methods In vitro study using the mouse liver NCTC-1469 cell line was conducted to estimate the cytotoxicity as well as the inhibitory effect of LF extract against alcohol-treated cell damage. In vivo study used an alcohol-fed Wister rat model orally administered EtOH (3.95 g/kg of body weight/d) with or without LF extract (100 or 200 mg/kg body weight) for 6 weeks. Serum and liver tissue were collected to evaluate hepatic injury and antioxidant-related enzyme activity. Results The EC50 value for the DPPH radical scavenging capacity of LF extract was 451.5 μg/mL, whereas the IC50 value of LF extract in terms of EtOH-induced reactive oxygen species (ROS) generation was 98.3 μg/mL without cell cytotoxicity. LF extract (200 mg/kg body weight) significantly reduced the triglyceride content of serum (33%) as well as hepatic lipid peroxidation (36%), whereas SOD activity was elevated three-fold. LF extract suppressed expression of CYP2E1 and TNF-α, and attenuated alcohol-induced abnormal morphological changes. Discussion and conclusion LF extract attenuated liver damage induced by alcoholic oxidative stress through inhibition of ROS generation, down-regulation of CYP2E1, and activation of hepatic antioxidative enzymes. Homeostasis of the antioxidative defence system in the liver by LF extract mitigated hepatic disorder following chronic alcohol intake.

Topics: Animals; Antioxidants; Asteraceae; Biphenyl Compounds; Cell Line; Cytochrome P-450 CYP2E1; Cytoprotection; Disease Models, Animal; Dose-Response Relationship, Drug; Lipid Peroxidation; Liver; Liver Diseases, Alcoholic; Male; Mice; Oxidative Stress; Phytotherapy; Picrates; Plant Extracts; Plant Leaves; Plants, Medicinal; Rats, Wistar; Reactive Oxygen Species; Superoxide Dismutase; Tumor Necrosis Factor-alpha

Context Cyclophosphamide (CTX) is used to treat different cancer types, although it causes severe hepatotoxicity due to its oxidative stress effect. Rosmarinus officinalis, L. (Lamiaceae) has a therapeutic potential against hepatotoxicity due to its antioxidant activity. Objective The objective of this study is to investigate the phytochemical analysis of the methanol extract of Rosmarinus officianalis leaves (MEROL) and its efficacy against CTX-induced hepatotoxicity. Materials and methods The phytochemical analyses were assessed spectrophotometericaly. To assess the MEROL efficacy, 72 Swiss albino mice were divided into six groups. Group 1 was control, groups 2 and 3 included mice which were injected intraperitoneally (i.p.) with 100 or 200 mg/kg of MEROL at days 1, 4, 7, 10, 13 and 16; group 4 was injected (i.p.) with CTX (200 mg/kg) at day 17, groups 5 and 6 were injected (i.p.) with MEROL as groups 3 and 4 followed by 200 mg/kg CTX at day 17, respectively. At day 22, six mice from each group were sacrificed and the others were sacrificed at day 37. Results MEROL has a high content of total phenolics, saponins, total antioxidant capacity and DPPH radical scavenging activity. The median lethal dose (LD50) value of MEROL was 4.125 g/kg b.w. The inhibitory concentration 50 (IC50) value for DPPH radical scavenging was 55 μg/mL. Pretreatment with 100 mg/kg MEROL for 16 d ameliorated CTX-induced hepatotoxicity represented in lowering the levels of the aspartate aminotransferase (AST) and lipid profile and minimizing the histological damage. Conclusions Pretreatment with 100 mg/kg b.w. MEROL mitigated CTX-induced hepatotoxicity due to its antioxidant activity.

Topics: Animals; Antioxidants; Biomarkers; Biphenyl Compounds; Chemical and Drug Induced Liver Injury; Cyclophosphamide; Disease Models, Animal; Lethal Dose 50; Liver; Male; Methanol; Mice; Phenols; Phytotherapy; Picrates; Plant Extracts; Plant Leaves; Plants, Medicinal; Rosmarinus; Saponins; Solvents; Spectrum Analysis; Time Factors

Context The present study deals with new biological properties of the wild edible Diplotaxis simplex (Viv.) Spreng (Brassicaceae). Objectives The current study evaluates the antioxidant, the anti-inflammatory and the anti-cancer properties of ethyl acetate and ethanol extracts from D. simplex flowers. Materials and methods The anti-proliferative activity of the extracts (10-70 μg/mL) was assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) against human colon cancer cell line Caco-2. The anti-inflammatory potential was evaluated by the inhibitory effect of the extracts (1.5-7.5 mg/mL) on phospholipase A2 activity as well as on carrageenan-induced paw oedema in mice. Extracts (200 mg/kg) or indomethacin (50 mg/kg) as positive control were injected intraperitoneally for albino mice prior to the induction of the oedema by carrageenan. Antioxidant activities were investigated using various complementary methods. Results Flower extracts contained a high level of polyphenolics (17.10-52.70 mg GAE/g) and flavonoids (74.20-100.60 mg QE/g), which correlate with its appreciable antioxidant potential in β-carotene peroxidation (IC50 value: 12.50-27.10 μg/mL), DPPH(•) radical-scavenging (IC50 value: 0.20-0.40 mg/mL), Fe(3+ )reducing (EC50 value: 0.10-0.14 mg/mL) and Fe(2+ )chelating (IC50 value: 0.20-0.60 mg/mL) assays. These extracts were effective in inhibiting cancer cell growth (IC50 value: 62.0-63.25 μg/mL). Besides, the ethyl acetate extract inhibited phospholipase A2 activity (IC50 value: 2.97 mg/mL) and reduced the paw oedema in mice (from 0.38 ± 0.01 to 0.24 ± 0.01 cm), 4 h post-carrageenan challenge. Conclusion These data suggest that D. simplex may be useful as a candidate in the treatment of inflammation and the colon cancer.

Topics: Acetates; Animals; Anti-Infective Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Biphenyl Compounds; Brassicaceae; Caco-2 Cells; Carrageenan; Cell Proliferation; Colonic Neoplasms; Disease Models, Animal; Dose-Response Relationship, Drug; Edema; Ethanol; Flowers; Humans; Inhibitory Concentration 50; Male; Mice; Phospholipase A2 Inhibitors; Phospholipases A2; Phytotherapy; Picrates; Plant Extracts; Plants, Medicinal; Solvents

The aim of the current study was to evaluate the antinociceptive activity of the selected Pakistani medicinal plants (Chenopodium botrys, Micromeria biflora and Teucrium stocksianum) in-vivo followed by their antioxidant potential against 1,1-diphenyl-2-picrylhidrazyl (DPPH) in-vitro. The results demonstrated profound antinociceptive effect of both the crude methanolic extract of Chenopodium botrys (CBM) and subsequent aqueous fraction (CBW) of C. botrys with 80.76% and 84% pain relief in acetic acid induced writhing test at 100 mg/kg i.p respectively. Similarly the crude methanolic extract of Micromeria biflora (MBM) and its subsequent aqueous fraction (MBW) with 66.46% 78.08% pain reversal in acetic acid induced writhing test respectively at 100mg/kg i.p. However, the crude methanolic extract and isolated water fraction of Teucrium stocksianum (TS) did not show any significant effect at test doses. Both the crude extracts and aqueous fractions of selected medicinal plants exhibited marked scavenging effects on DPPH and therefore strongly support the antinociceptive activity. Phytochemical analysis indicated the presence of various classes of natural products (alkaloids, terpenoids, flavonoids etc.) and thus the current finding can be attributed to the presence of these compounds. In short, our findings provide a strong scientific background to the folk uses C. botrys and M. biflora in the management of various painful conditions.

Topics: Acetic Acid; Analgesics; Animals; Antioxidants; Biphenyl Compounds; Chenopodium; Disease Models, Animal; Dose-Response Relationship, Drug; Lamiaceae; Methanol; Mice, Inbred BALB C; Pain; Pakistan; Phytochemicals; Phytotherapy; Picrates; Plant Extracts; Plants, Medicinal; Solvents; Teucrium; Water

Alnus species have been used for the treatment of rheumatism, hemorrhoids and for wound healing in folk medicine.. Aqueous and methanol extracts of A. glutinosa (L.) Gaertner subsp. glutinosa, A. orientalis Decne. var. orientalis and A. orientalis var. pubescens Dippel leaves were evaluated for their wound healing, anti-inflammatory and antioxidant activities. In vivo wound models of linear incision and circular excision were performed. "Inhibition of acetic acid-induced capillary permeability", "carrageenan-induced hind paw edema" and T"PA-induced ear edema" assays were applied to determine the anti-inflammatory effects. For the antioxidant activity assessment, DPPH and ABTS radicals scavenging effect, reducing power and denaturation of nonspecific hydroxyl radical-targeted 2-deoxyribose were used. In vitro inhibitory effects on enzymes hyaluronidase, collagenase and elastase were evaluated. The methanol extract of the leaves of A. glutinosa subsp. glutinosa (MB), the most potent extract, was fractionated by bioassay-guided fractionation technique. The structure of the isolated compound was determined as shikimic acid by using NMR and IR analyses.. MB increased the wound tension by 42.79% value and provided a contraction by 51.58%. Wound tension, contraction capacity and tissue hydroxyproline levels were increased with the application of the fraction EtOAc: MeOH (Fr. D), subfraction D. This is the first and unique study that investigates wound healing, anti-inflammatory and antioxidant effects of some Alnus taxons growing in Turkey. According to the results, shikimic acid was found to be the major compound responsible from the activity.

Topics: Alnus; Animals; Anti-Inflammatory Agents; Antioxidants; Benzothiazoles; Biphenyl Compounds; Capillary Permeability; Carbon-13 Magnetic Resonance Spectroscopy; Carrageenan; Disease Models, Animal; Edema; Glycoside Hydrolase Inhibitors; Hyaluronoglucosaminidase; Male; Methanol; Mice; Phytochemicals; Picrates; Plant Extracts; Plant Leaves; Proton Magnetic Resonance Spectroscopy; Rats, Sprague-Dawley; Shikimic Acid; Solvents; Spectrophotometry, Infrared; Sulfonic Acids; Tetradecanoylphorbol Acetate; Water; Wound Healing

Ethanoic extracts from the fruiting bodies and mycelia of the elm oyster mushroom, Hypsizygus ulmarius, were evaluated for their antioxidant, anti-inflammatory, and antitumor properties. Ethnolic extracts of fruiting body and mycelia showed 88%, 85%, 71%, and 85%, 65%, 70% 2,2-diphenyl-1-picrylhydrazyl, hydroxyl (DPPH) and 2,2'-azinobis (3-ethyl benzothiazolin-6-sulfonic acid) (ABTS) radical-scavenging activities, respectively, at a concentration of 1000 µg/mL. The anti-inflammatory activity was determined using carrageenan- and formalin- induced paw edema models. Diclofenac was used as the standard drug. In both models, the mycelia extract showed higher activity than the fruiting body extract. The antitumor effect of the extracts against Dalton's Lymphoma Ascites cell-line-induced tumors showed significant antitumor activity. Mycochemical analysis confirmed the presence of many pharmacologically active compounds such as phenol, alkaloids, proteins, tannins, and polysaccharides. Among these, polysaccharides and phenolic compounds were present at a higher concentration in both extracts. These compounds might be largely responsible for the mushroom's medicinal properties. The results of this study indicate that H. ulmarius possesses significant antioxidant, anti-inflammatory, and antitumor properties.

Topics: Agaricales; Animals; Anti-Inflammatory Agents; Antineoplastic Agents; Antioxidants; Benzothiazoles; Biphenyl Compounds; Complex Mixtures; Diclofenac; Disease Models, Animal; Edema; Fruiting Bodies, Fungal; Male; Mice; Mycelium; Picrates; Sulfonic Acids

Here, we evaluate the anti-inflammatory and wound-healing effects of methanolic crude extract obtained from aerial parts (leaves and branches) of Rubus imperialis Chum. Schl. (Rosaceae) and the pure compound niga-ichigoside F1. Anti-inflammatory activity was determined in vivo and in vitro, and the healing effect was evaluated in surgical lesions in mice skin. The 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) assay and H

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Carrageenan; Cell Line; Chemotaxis, Leukocyte; Disease Models, Animal; Dose-Response Relationship, Drug; Hydrogen Peroxide; Inflammation; Lipopolysaccharides; Macrophages, Peritoneal; Male; Methanol; Mice, Inbred BALB C; Neutrophil Infiltration; Neutrophils; Oxidative Stress; Phytotherapy; Picrates; Plant Components, Aerial; Plant Extracts; Plants, Medicinal; Rubus; Saponins; Skin; Solvents; Wound Healing; Wounds, Penetrating

The leaves of Allophylus edulis (A. St.-Hil., A. Juss. & Cambess.) Radlk. (Sapindaceae) are traditionally used as a natural anti-inflammatory agent; however, there are no scientific studies demonstrating its activity essential oil. The content of essential oil in A. edulis may be the chemical basis to explain its ethnobotanical uses, since infusions of this plant are used to treat inflammation in the traditional medicine in Brazil.. This study evaluated the anti-inflammatory, antioxidant and anti-mycobacterial activities of the essential oil (EOAE) and viridiflorol, its main compound.. Essential oil from fresh leaves of A. edulis (EOAE) was obtained by hydrodistillation in a Clevenger-type apparatus. Forty-one compounds, accounting for 99.10% of the oil, were identified by gas chromatography-mass spectrometry (GC-MS). The major constituent of the oil was viridiflorol (30.88%). Additionally, the essential oil and viridiflorol were evaluated using an in vitro test against Mycobacterium tuberculosis and in 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) assays. Both EOAE (30 and 100mg/kg) and viridiflorol (3 and 30mg/kg) by oral administration were assayed in carrageenan-induced mice paw oedema and pleurisy using subcutaneous injection of dexamethasone (0.5mg/kg) as the positive control.. EOAE and viridiflorol displayed moderate in vitro activity in the M. tuberculosis assay. In all tests, EOAE and viridiflorol showed moderate antioxidant activity compared with reference standards. Both EOAE and viridiflorol showed significant inhibition in the carrageenan-induced mice paw oedema via oral administration of the oil (30 and 100mg/kg), compound (3 and 30mg/kg), and subcutaneous injection of dexamethasone (0.5mg/kg, reference drug). Also EOAE and viridiflorol significantly inhibited carrageenan (Cg) induced pleurisy, reducing the migration of total leucocytes in mice by 62±5% (30mg/kg of oil), 35±8% (100mg/kg of oil), 71±5% (3mg/kg of viridiflorol) and 57±3% (30mg/kg of viridiflorol).. For the first time, the results from this work corroborate the literature, showing that A. edulis can be used as a natural anti-inflammatory agent. Moreover, both EOAE and viridiflorol exhibited biological activities, such as anti-mycobacterial, anti-inflammatory and antioxidant activity.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Antitubercular Agents; Benzothiazoles; Biphenyl Compounds; Carrageenan; Chemotaxis, Leukocyte; Dexamethasone; Disease Models, Animal; Dose-Response Relationship, Drug; Edema; Female; Gas Chromatography-Mass Spectrometry; Male; Mice; Mycobacterium tuberculosis; Oils, Volatile; Phytotherapy; Picrates; Plant Extracts; Plant Leaves; Plant Oils; Plants, Medicinal; Pleurisy; Sapindaceae; Sulfonic Acids; Terpenes; Time Factors

Caesalpinia mimosoides Lam. is one of the important traditional folk medicinal plants in the treatment of skin diseases and wounds used by healers of Uttara Kannada district of Karnataka state (India). However scientific validation of documented traditional knowledge related to medicinal plants is an important path in current scenario to fulfill the increasing demand of herbal medicine.. The study was carried out to evaluate the claimed uses of Caesalpinia mimosoides using antimicrobial, wound healing and antioxidant activities followed by detection of possible active bio-constituents.. Extracts prepared by hot percolation method were subjected to preliminary phytochemical analysis followed by antimicrobial activity using MIC assay. In vivo wound healing activity was evaluated by circular excision and linear incision wound models. The extract with significant antimicrobial and wound healing activity was investigated for antioxidant capacity using DPPH, nitric oxide, antilipid peroxidation and total antioxidant activity methods. Total phenolic and flavonoid contents were also determined by Folin-Ciocalteu, Swain and Hillis methods. Possible bio-active constituents were identified by GC-MS technique. RP-UFLC-DAD analysis was carried out to quantify ethyl gallate and gallic acid in the plant extract.. Preliminary phytochemical analysis showed positive results for ethanol and aqueous extracts for all the chemical constituents. The ethanol extract proved potent antimicrobial activity against both bacterial and fungal skin pathogens compared to other extracts. The efficacy of topical application of potent ethanol extract and traditionally used aqueous extracts was evidenced by the complete re-epithelization of the epidermal layer with increased percentage of wound contraction in a shorter period. However, aqueous extract failed to perform a consistent effect in the histopathological assessment. Ethanol extract showed effective scavenging activity against DPPH and nitric oxide free radicals with an expressive amount of phenolic and moderate concentration of flavonoid contents. Ethyl gallate and gallic acid were found to be the probable bio-active compounds evidenced by GCMS and RP-UFLC-DAD analysis.. The study revealed the significant antimicrobial, wound healing and antioxidant activities of tender parts of C. mimosoides and proved the traditional folklore knowledge.

Topics: Animals; Anti-Infective Agents; Antioxidants; Biphenyl Compounds; Caesalpinia; Disease Models, Animal; Female; India; Lipid Peroxidation; Male; Medicine, Traditional; Microbial Sensitivity Tests; Picrates; Plant Extracts; Plant Leaves; Plant Shoots; Plants, Medicinal; Rats, Wistar; Skin; Skin Diseases; Wound Healing

Ocimum species are traditionally used for the treatment of anxiety, nerve pain, convulsions and a variety of neurodegenerative disorders. The present study was undertaken to evaluate the anti-amnesic effect of O. basilicum L., O. sanctum L. and O. gratissimum L. extracts using in-vitro and in-vivo models.. In-vitro acetylcholinesterase (AChE) inhibitory and antioxidant activities of hydro-methanol extracts of plants were evaluated using Ellman and DPPH and FRAP assays, respectively. The most active extract i.e. O. basilicum extract (OBE) was further explored for the possible anti-amnesic activity in mouse model of scopolamine induced amnesia using behavioral models (elevated plus maze and passive shock avoidance task). Brain AChE activity, oxidative profile and histopathological studies were assessed to outline the anti-amnesic mechanism of the extract.. OBE possesses antioxidant and AChE inhibitory activity. These biochemical changes are responsible for the anti-amnesic and neuroprotective activities of O. basilicum which may be attributed to the presence of phenolic and flavonoid compounds. This can be developed as an effective anti-amnesic drug.

Topics: Acetylcholinesterase; Amnesia; Animals; Antioxidants; Avoidance Learning; Behavior, Animal; Biphenyl Compounds; Cerebral Cortex; Cholinesterase Inhibitors; Chromatography, High Pressure Liquid; Cognition; Disease Models, Animal; Dose-Response Relationship, Drug; Female; GPI-Linked Proteins; Hippocampus; Male; Maze Learning; Memory; Methanol; Mice, Inbred BALB C; Neuroprotective Agents; Ocimum; Ocimum basilicum; Ocimum sanctum; Phenols; Phytotherapy; Picrates; Plant Extracts; Plant Leaves; Plants, Medicinal; Reaction Time; Scopolamine; Solvents; Time Factors

The leaves of Vitis vinifera is used in traditional medicine for diarrhea, hepatitis and stomachaches. The objective of this study was to investigate the anti-oxidant, anti-inflammatory, analgesic and antipyretic properties of the hydroalcoholic leaf extract of Vitis vinifera (EVV) on experimental models to provide scientific basis for its use.. The EVV was chemically characterized by LC-MS/MS analyses. The in vitro antioxidant activities of the EVV extract were measured using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay and Ferric reducing antioxidant power assay (FRAP). Analgesic activity using acetic acid induced writhing and formalin test in mice, anti-inflammatory activity using carrageenan induced paw oedema and acetic acid-induced vascular permeability in mice, and antipyretic activity using Brewer's yeast induced pyrexia in rats were evaluated at 100mg/kg, 200mg/kg, and 400mg/kg doses of the extract.. The extract (EVV) was found to contain resveratrol, quercetin, catechin, flavone, flavonols, anthocyanin, gallic acid and epicatechin. EVV produced significant dose-response anti-inflammatory activity against carrageenan-induced paw edema. EVV at dosages of 100, 200 and 400mg/kgbw significantly reduced carrageenan-induced paw edema by 34.48% (P<0.05), 36.20% (P<0.05), and 41.37% (P<0.05) at 5h after carrageenan injection, respectively. Also EVV extract reduces significantly acetic acid-induced vascular permeability in mice dose dependently. EVV (100, 200 and 400mg/kgbw) produced significant dose-response analgesic activity in the formalin test. However, the low percentage inhibition (50%) suggests that it is not a centrally acting analgesic. Extract at dosages of 100, 200 and 400mg/kg bw, p.o. significantly reduced acetic acid-induced writhing by 48.15% (p<0.05), 57.97% (p<0.05), and 68.09% (p<0.05), respectively. The extract also caused marked dose-dependent inhibition of formalin-induced pain in the second phase (p<0.05). Statistical significant reduction in rectal temperatures was observed in standard group at 21 and 23h, and in 200mg/kg and 400mg/kg doses of the extract at 23h (p<0.05) compared with the 19h.. The results obtained indicated potential analgesic, anti-inflammatory and antipyretic effects of them hydroalcoholic leaf extract of V. vinifera observed at doses tested which support the claim for the traditional use of the plant in the treatment of various inflammatory and pain diseases.

Topics: Acetic Acid; Analgesics; Animals; Anti-Inflammatory Agents; Antioxidants; Antipyretics; Behavior, Animal; Biphenyl Compounds; Body Temperature Regulation; Capillary Permeability; Carrageenan; Chromatography, Liquid; Disease Models, Animal; Dose-Response Relationship, Drug; Edema; Ethanol; Ferricyanides; Fever; Formaldehyde; Mice; Molecular Structure; Pain; Phytotherapy; Picrates; Plant Extracts; Plant Leaves; Plants, Medicinal; Saccharomyces cerevisiae; Solvents; Tandem Mass Spectrometry; Vitis

Obesity is a one of the main global public health problems associated with chronic diseases such as coronary heart disease, diabetes and cancer. As a solution to obesity, we suggest Plantago albicans, which is a medicinal plant with several biological effects. This study assesses the possible anti-obesity protective properties of Plantago albicans in high fat diet-fed rats. 28 male Wistar rats were divided into 4 groups; a group which received normal diet (C), the second group was fed HDF diet (HDF), the third group was given normal diet supplemented with Plantago albicans (P.AL), and the fourth group received HDF supplemented with Plantago albicans (HDF+P.AL) (30mg/kg/day) for 7 weeks. Our results showed an increase in body weight of HDF rats by ∼16% as compared to the control group with an increase in the levels of total cholesterol (TC) as well as LDL-cholesterol, triglycerides (TG) in serum. Also, the concentration of TBARS increased in the liver and heart of HDF-fed rats as compared to the control group. The oral gavage of Plantago albicans extract to obese rats induced a reduction in their body weight, lipid accumulation in liver and heart tissue, compared to the high-fat diet control rats. The obtained results proved that the antioxidant potency of Plantago albicans extracts was correlated with their phenolic and flavonoid contents. The antioxidant capacity of the extract was evaluated by DPPH test (as EC50=250±2.12μg/mL) and FRAP tests (as EC50=27.77±0.14μg/mL). These results confirm the phytochemical and antioxidant impact of Plantago albicans extracts. Plantago albicans content was determined using validated HPLC methodology.

Topics: Animals; Anti-Obesity Agents; Antioxidants; Biomarkers; Biphenyl Compounds; Chromatography, High Pressure Liquid; Diet, High-Fat; Disease Models, Animal; Flavonoids; Fluorescence Recovery After Photobleaching; Lipids; Liver; Male; Myocardium; Obesity; Phenols; Phytotherapy; Picrates; Plant Extracts; Plant Leaves; Plantago; Plants, Medicinal; Rats, Wistar; Weight Gain

Paeonia lactiflora and P. obovata are perennial herbs, each root of which has been consumed as a major oriental medicine, Paeoniae Radix and a famous folk medicine, Mountain Paeony Root, respectively. Although morphological studies have been performed comparing these two plants, there is insufficient scientific evidence that characterizes the differences in their chemical profiles and biological activities. Hence, the present study was undertaken to compare these two medicinal foods using a high-performance liquid chromatography-diode-array detector (HPLC-DAD) analysis and a gastric ulcer model in mice. HPLC analysis employed to assess the nine components revealed that P. lactiflora exhibited higher contents of phenolic compounds than P. obovata. Although a monoterpene glycoside, 6'-O-acetylpaeoniflorin was identified in P. obovata, it was not detected in P. lactiflora. Multivariate statistical analysis for HPLC data revealed that the orthogonal projections to latent structure-discriminant analysis is more appropriate than principal component analysis for differentiating the two groups. Moreover, the 50% methanol P. lactiflora extract (PL) was more effective against experimental gastric ulcer than P. obovata extract (PO) in the HCl/ethanol-induced ulcer model. In addition, PL displayed higher 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity and lower nitric oxide production in a murine macrophage cell line, RAW 264.7, than PO. The DPPH radical scavenging activity of PL was as high as that of the positive control, butylated hydroxytoluene, at a concentration of 25 μg/mL.

Topics: Animals; Biphenyl Compounds; Butylated Hydroxytoluene; Cell Line; Chromatography, High Pressure Liquid; Disease Models, Animal; Drugs, Chinese Herbal; Ethanol; Glycosides; Indicators and Reagents; Male; Mice; Mice, Inbred ICR; Monoterpenes; Nitric Oxide; Paeonia; Phenol; Phytotherapy; Picrates; Plant Extracts; Plant Roots; Stomach Ulcer

Background. Liver diseases still represent a major health burden worldwide. Moreover, medicinal plants have gained popularity in the treatment of several diseases including liver. Thus, the present study was to evaluate the effectiveness of Piper cubeba fruits in the amelioration of CCl4-induced liver injuries and oxidative damage in the rodent model. Methods. Hepatoprotective activity was assessed using various biochemical parameters like SGOT, SGPT, γ-GGT, ALP, total bilirubin, LDH, and total protein. Meanwhile, in vivo antioxidant activities as LPO, NP-SH, and CAT were measured in rat liver as well as mRNA expression of cytokines such as TNFα, IL-6, and IL-10 and stress related genes iNOS and HO-1 were determined by RT-PCR. The extent of liver damage was also analyzed through histopathological observations. Results. Treatment with PCEE significantly and dose dependently prevented drug induced increase in serum levels of hepatic enzymes. Furthermore, PCEE significantly reduced the lipid peroxidation in the liver tissue and restored activities of defense antioxidant enzymes NP-SH and CAT towards normal levels. The administration of PCEE significantly downregulated the CCl4-induced proinflammatory cytokines TNFα and IL-6 mRNA expression in dose dependent manner, while it upregulated the IL-10 and induced hepatoprotective effect by downregulating mRNA expression of iNOS and HO-1 gene.

Topics: Animals; Antioxidants; Biphenyl Compounds; Carbon Tetrachloride; Catalase; Chemical and Drug Induced Liver Injury; Cytokines; Disease Models, Animal; Ethanol; Free Radical Scavengers; Lignans; Liver; Male; Malondialdehyde; Oxidative Stress; Phytochemicals; Picrates; Piper; Plant Extracts; Protective Agents; Rats, Wistar; RNA, Messenger; Sulfhydryl Compounds

Wild carrot, Daucus carota L. ssp. carota (Apiacae), is widely distributed throughout the world and has various uses in traditional medicine in Lebanon.. The present study aimed to fractionate and analyze the chemical composition of the Daucus carota oil extract (DCOE) fractions and to evaluate their antioxidant and hepatoprotective properties in vitro and in vivo.. DCOE was chromatographed on silica gel column to produce four fractions: pentane (F1), 50:50 pentane:diethyl ether (F2), diethyl ether (F3), and 93:7 chloroform: methanol (F4). Qualitative and quantitative analyses of oil fractions were performed by GC-MS and HPLC techniques. The in vitro antioxidant properties were assessed using DPPH, FIC, and ferric-reducing antioxidant power (FRAP) assays. The hepatoprotective property was determined by examining the levels of serum markers (alanine transaminase (ALT) and aspartate transaminase (AST)) and hepatic antioxidant (superoxide dismutase (SOD), catalase (CAT), and glutathione-S-transferase (GST)) enzymes in CCl4-intoxicated mice pretreated with intraperitoenal 50, 100, or 200 mg/kg b.w. of the oil fractions for 5 d.. GCMS analysis of F2 revealed the presence of 2-himachalen-6-ol (61.4%) which is reported for the first time in Daucus carota species. F3 and F4 were rich in phenolics and flavonoids and demonstrated significant DPPH activity (IC50 = 0.29 and 0.38 mg/ml, respectively) and high FRAP values (225.11 and 437.59 µmol FeSO4/g, respectively). The sesquiterpene-rich fraction F1 had the highest FIC ability (IC50 = 0.28 mg/ml). Pretreatment with F1 and F4 reversed the CCl4-induced decrease in SOD, CAT, and GST levels and reduced significantly hepatic damage.. The current results suggested that wild carrot oil fractions exhibited a unique chemical composition and possessed significant antioxidant activities as well as hepatoprotective effects against CCl4-induced hepatotoxicity.

Topics: Animals; Antioxidants; Biomarkers; Biphenyl Compounds; Carbon Tetrachloride; Chemical and Drug Induced Liver Injury; Chemical Fractionation; Chromatography, High Pressure Liquid; Cytoprotection; Daucus carota; Disease Models, Animal; Dose-Response Relationship, Drug; Enzymes; Gas Chromatography-Mass Spectrometry; Liver; Mice, Inbred BALB C; Oxidation-Reduction; Phytotherapy; Picrates; Plant Extracts; Plant Oils; Plants, Medicinal

In the present study, we describe the synthesis of a new set of 1,2,4-triazolo[1,5-a]pyridines and their fused ring systems. The products were assayed for various types of biological activities like anti-inflammatory and antioxidative activity. Compounds 4c, 4f, 12a, 14, 16, and 19 were found to reduce carrageenan- and dextran-induced inflammation in rats. In addition, compounds 4f and 12a were found to have antioxidative radical scavenging activity. Furthermore, these compounds were tested in the model system Caenorhabiditis elegans and there increased heat stress resistance, reduced the formation of advanced glycation end products, and finally extended the life span.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Caenorhabditis elegans; Carrageenan; Dextrans; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Design; Edema; Glycation End Products, Advanced; Glycosylation; Heat-Shock Response; Longevity; Male; Molecular Structure; Oxidative Stress; Picrates; Pyridines; Rats; Structure-Activity Relationship; Time Factors; Triazoles

3-O-demethylswertipunicoside (3-ODS) has been reported to protect dopaminergic neurons against neurotoxicity induced by 1-methyl-4-phenylpyridinium (MPP(+)) in PC12 cells. Here, we investigate the neuroprotective effects in vivo and antioxidant activities in vitro of 3-ODS. In the 1-methyl-4-phenyl-1,2,3,6- tetrahydropyridine (MPTP)-treated mouse model of Parkinson's disease (PD), 3-ODS dose-dependently improved motor coordination (as shown by rotarod test), increased the contents of dopamine (DA) and its metabolites in the striatum, and increased the number of tyrosine hydroxylase (TH)-positive neurons in the substantia nigra (SN). In addition, 3-ODS also increased the spine density in hippocampal CA1 neurons. In antioxidant assays, 3-ODS showed a strong capacity in scavenging hydroxyl radical, superoxide anion and 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical in a concentration-dependent manner. Taken together, we conclude that 3-ODS attenuates the PD-related motor deficits mainly through its neuroprotective effects, growth-promoting effects on spine density, and its antioxidant activities.

Topics: 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine; 3,4-Dihydroxyphenylacetic Acid; Animals; Biphenyl Compounds; Disease Models, Animal; Dopamine; Dose-Response Relationship, Drug; Glucosides; Hippocampus; Hydroxyl Radical; In Vitro Techniques; Male; Mice; Mice, Inbred C57BL; Motor Activity; MPTP Poisoning; Neuroprotective Agents; Picrates; Spine; Superoxides; Tyrosine 3-Monooxygenase; Xanthones

Our study aimed to investigate the antidepressant-like effect of ethyl acetate extract of the flowers of Campsis grandiflora (EFCG) in a mice model of chronic unpredictable mild stress (CUMS).. HPLC-Q-TOF-MS was used to identify the chemical constituents of EFCG. The DPPH assay and ABTS radical-scavenging assay were performed to measure the antioxidant properties. The protective properties of EFCG against H2 O2 -induced oxidative damage were analysed in PC12 cells. The changes of behaviour profiles were investigated by using open-field test, sucrose preference test, forced swimming test (FST) and tail suspension test (TST). Brain tissue samples of mice were collected, and antioxidative measure levels were measured.. The result showed that EFCG had the most active anti-oxidative effect and the protective effect against H2 O2 oxidative injury in PC12 cells. Treatment with the EFCG significantly reduced the depressant-like severity and immobility period as compared with untreated CUMS mice in FST and TST. Moreover, EFCG significantly elevated the contents of superoxide dismutase, Glutathione Peroxidase and decreased the contents of Malonaldehyde (MDA) in mice brain.. Our study found first the antidepressant activity of the EFCG. The results suggested the therapeutic potential of EFCG for depressive disorder.

Topics: Acetates; Animals; Antidepressive Agents; Antioxidants; Behavior, Animal; Benzothiazoles; Bignoniaceae; Biphenyl Compounds; Brain; Chromatography, High Pressure Liquid; Disease Models, Animal; Flowers; Food Preferences; Male; Mice; Motor Activity; Oxidative Stress; PC12 Cells; Phytotherapy; Picrates; Plant Extracts; Plants, Medicinal; Rats; Solvents; Spectrometry, Mass, Electrospray Ionization; Stress, Psychological; Sulfonic Acids; Swimming

Allergic dermatitis among common skin diseases is a chronic and recurrent inflammatory skin disorder caused by genetic, environmental, allergens as well as microbial factors. Allergic dermatitis patients clinically present skin erythematous plaques, eruption, elevated serum immunoglobulin E (IgE) and T helper cell type 2 (Th2) cytokine levels. The leaf of walnut tree Juglans mandshurica Maxim (JM) is consumed food and traditional phytomedicine in Asia, China, Siberia and Korea. JM has been reported to have various pharmacological activities, such as anti-tumor, anti-oxidative, and anti-bacterial effects. However, no study of the inhibitory effects of JM on allergic dermatitis has been reported. Here, we demonstrated the effect of JM against 2,4-dinitrochlorobenzene-induced allergic dermatitis-like skin lesions. 0.5% JM or 1% dexamethasone (positive control) applied to the dorsal skin inhibited development of allergic dermatitis-like skin lesions and scratching behavior. Moreover, the Th2-mediated inflammatory cytokines IgE, tumor necrosis factor-α, interleukin (IL)-1, and IL-13, were significantly reduced by JM treatment. Thus JM can inhibit development of allergic dermatitis-like skin lesions in mice by regulating immune mediators, and may be an effective alternative therapy for allergic dermatitis.

Topics: Animals; Anti-Allergic Agents; Behavior, Animal; Biphenyl Compounds; Cytokines; Dermatitis, Allergic Contact; Dinitrochlorobenzene; Disease Models, Animal; Free Radical Scavengers; Immunoglobulin E; Juglans; Male; Mice; Mice, Inbred ICR; Picrates; Plant Extracts; Plant Leaves; Th2 Cells

Gynura segetum, family Compositae, is a cultivated species and can be found growing in the tropical regions of Indonesia and Malaysia. The plant is known for its use for the treatment of cancer, inflammation, diabetes, hypertension and skin afflictions. In the current study, in vivo anti-inflammatory effect of the methanol extract G. segetum leaf and its antioxidant effect in vitro have been investigated for the first time. The in vitro antioxidant activities of the methanol extract were measured using common methods including total phenolic content; total flavonoid content; scavenging of 1,1-diphenyl-2-picrylhydrazyl (DPPH) and β-carotene bleaching assays. The in vivo anti-inflammatory activities were tested using the cotton pellet implanted animal model. The measurement of pro-inflammatory cytokine (TNF-α and IL-1) levels in the blood samples of the rats was carried out by using ELISA kits. The inhibitory activity on cyclooxygenase (COX) enzyme of methanol extract was also evaluated. The methanol extract exhibited good antioxidant activity which is associated with their total phenolic and flavonoid contents. Methanol extract strongly inhibited the granuloma tissue formation in rats and the anti-inflammatory potential was mediated through the inhibition of pro-inflammatory cytokines and COX-2 enzyme activities. Taken together, the present study suggests that G. segetum's leaf is a natural source of antioxidants and has potential therapeutic benefits against chronic inflammation.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Asteraceae; Biphenyl Compounds; Cyclooxygenase 2; Disease Models, Animal; Flavonoids; Granuloma; Humans; Interleukin-1beta; Male; Methanol; Phenols; Phytotherapy; Picrates; Plant Extracts; Plant Leaves; Rats; Rats, Sprague-Dawley; Tumor Necrosis Factor-alpha

Spinal cord injury (SCI)-induced secondary oxidative stress associates with a clinical complication and high mortality. Treatments to improve the neurological outcome of secondary injury are considered as important issues. The objective of the current study is to evaluate the anti-oxidative effect of Tithonia diversifolia ethanolic extracts (TDE) on cells and apply the pharmacological effect to SCI model using a MRI imaging algorism.. The anti-oxidation properties were tested in a 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay. Rat liver cells (clone-9) were treated with various doses of TDE (0 ~ 50 μg/ml) before exposed to 250 μM H2O2 and cell survival was determined by MTT and LDH assays. We performed water apparent diffusion coefficient (ADC) map in MR techniques to investigate the efficacy of TDE treatment on SCI animal model. We performed T5 laminectomy and compression (50 g, 1 min) to induce SCI. PHILIP 3.0 T MRI was used to image 24 male Sprague-Dawley rats weighing 280-320 g. Rats were randomly divided into three groups: sham group, SCI group, SCI treated with TDE group. The MRI images were taken and ADC were acquired before and after of treatment of TDE (50 mg/kg B. W. orally, 5 days) in SCI model.. TDE protected clone-9 cells against H2O2-induced toxicity through DPPH scavenging mechanism. In addition, SCI induced the increase in ADC after 6 hours. TDE treatment slightly decreased the ADC level after 1-week SCI compared with control animals.. Our studies have proved that the cytoprotection effect of TDE, at least in part, is through scavenging ROS to eliminate intracellular oxidative stress and highlight a potential therapeutic consideration of TDE in alternative and complementary medicine.

Topics: Animals; Asteraceae; Biphenyl Compounds; Cells, Cultured; Diffusion; Disease Models, Animal; Hydrogen Peroxide; In Vitro Techniques; Magnetic Resonance Imaging; Male; Oxidative Stress; Phytotherapy; Picrates; Plant Extracts; Rats; Rats, Sprague-Dawley; Spinal Cord Injuries; Water

Acute hepatic inflammation is regarded as a hallmark of early stage fibrosis, which can progress to extensive fibrosis and cirrhosis. Sinapic acid is a phenylpropanoid compound that is abundant in cereals, nuts, oil seeds, and berries and has been reported to exhibit a wide range of pharmacological properties. In this study, we investigated the anti-inflammatory effect of sinapic acid in carbon tetrachloride (CCl4)-induced acute hepatic injury in rats. Sinapic acid was administered orally (10 or 20 mg/kg) to rats at 30 min and 16 h before CCl4 intoxication. Sinapic acid treatment of rats reduced CCl4-induced abnormalities in liver histology, serum alanine transaminase and aspartate transaminase activities, and liver malondialdehyde levels. In addition, sinapic acid treatment significantly attenuated the CCl4-induced production of inflammatory mediators, including tumor necrosis factor-alpha and interleukin-1β mRNA levels, and increased the expression of nuclear factor-kappa B (NF-κB p65). Sinapic acid exhibited strong free radical scavenging activity in vitro. Thus, sinapic acid protected the rat liver from CCl4-induced inflammation, most likely by acting as a free radical scavenger and modulator of NF-κB p65 activation and proinflammatory cytokine expression. Sinapic acid may thus have potential as a therapeutic agent for suppressing hepatic inflammation.

Topics: Acute Disease; Animals; Anti-Inflammatory Agents; Biphenyl Compounds; Blotting, Western; Body Weight; Carbon Tetrachloride; Chemical and Drug Induced Liver Injury; Coumaric Acids; Disease Models, Animal; Free Radical Scavengers; Interleukin-1beta; Lipid Peroxidation; Liver; Liver Function Tests; Male; Molecular Structure; Organ Size; Picrates; Rats; Rats, Sprague-Dawley; Reverse Transcriptase Polymerase Chain Reaction; Transcription Factor RelA; Transforming Growth Factor beta1

Ficus religiosa L. (Moraceae) is widely planted in the tropics. Its chemical constituents include tannin, saponin gluanol acetate, β-sitosterol, leucoanthocyanidin and leucoanthocyanin which are used for the treatment of pain, inflammation, impotence, menstrual disturbances, uterine tonic and urine related problems.. To determine the possible nephroprotective and curative effects of F. religiosa latex methanol extract against cisplatin induced acute renal failure.. Methanol extract was obtained by maceration process. Rats were divided in five groups. Group 1 was administered acacia (2% w/v) of 5 ml/kg throughout the experiment; group 2 was treated with single dose of cisplatin (5 mg/kg i.p.) on the 1st day; group 3 (200 mg/kg p.o.) of extract control for the 1st to 10th day, group 4 (200 mg/kg p.o.) of extract from the 1st to 10th day and a single dose of cisplatin (5 mg/kg, i.p.) on 11th day while group 5 received the same dose of cisplatin on day 1 and extract (200 mg/kg p.o.) from the 7th to 16th day.. Phytochemical screening of the extract revealed the presence of glycoside, alkaloids, tannins (phenolic compounds), flavonoids and amino acids. The half maximal inhibitory concentration (IC50) values of the extract were 31.75 ± 0.12 and 18.35 ± 0.48 µg/ml, respectively. The cisplatin-treated group 2 showed significant changes; renal functions, biochemical parameters and histopathology were significantly (**p < 0.01) recovered by 200 mg/kg curative and protective groups.. These findings demonstrated that F. religiosa latex and constituents have excellent nephroprotective and curative activities and thus have great potential as a source for natural health products.

Topics: Acute Kidney Injury; Administration, Oral; Animals; Antioxidants; Biphenyl Compounds; Cisplatin; Cytoprotection; Disease Models, Animal; Dose-Response Relationship, Drug; Ficus; Kidney; Lethal Dose 50; Lipid Peroxidation; Male; Methanol; Oxidative Stress; Phytotherapy; Picrates; Plant Extracts; Plants, Medicinal; Rats; Rats, Wistar; Solvents; Time Factors

Arthritis is inflammation of one or more joints. Terminalia chebula Retz. (Combretaceae) fruit is mentioned in Ayurveda as useful in treating arthritic disorders.. This work was undertaken to evaluate the anti-inflammatory, antioxidant, anti-lipid peroxidative and membrane-stabilizing effects of hydroalcoholic extract of Terminalia chebula fruits and also to establish a possible association between them.. In vivo anti-inflammatory activity of T. chebula fruit extract at different doses ranged from 50 to 500 mg/kg, p.o. was evaluated against carrageenin-induced inflammation in rats. Human erythrocyte hemolytic assay was used for in vitro anti-inflammatory activity testing with 50 to 500 µg/ml fruit extract. Antioxidant potential of test fruit extract (10 to 100 µg/ml) was evaluated using TBARS and DPPH methods. The fruit extract was standardized for total phenolic content using Folin-Ciocalteu method.. The standardized extract at 250 mg/kg, p.o. dose caused 69.96% reduction in carrageenin-induced rat paw edema and demonstrated 96.72% protective effect on human RBC membrane stability. Besides, T. chebula fruit extract significantly reduced the in vivo formation of TBARS in carrageenin-induced rat liver with IC50 94.96 mg/kg, p.o. and also in vitro radical scavenging activities in DPPH assay method with IC50 42.14 µg/ml. The standardized extract contains phenolics 118.5 mg gallic acid equivalent/g of extract.. These promising findings support the traditional use of T. chebula fruits in the treatment of arthritic disorders and suggest that radical quenching may be one of the mechanisms for its anti-inflammatory activity.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Biphenyl Compounds; Cells, Cultured; Disease Models, Animal; Dose-Response Relationship, Drug; Edema; Erythrocyte Membrane; Erythrocytes; Ethanol; Female; Free Radicals; Fruit; Hemolysis; Humans; Lipid Peroxidation; Liver; Male; Malondialdehyde; Medicine, Ayurvedic; Picrates; Rats; Rats, Wistar; Terminalia; Water

context: Stems and leaves of Pittocaulon spp. (Asteraceae) are used in Mexican traditional medicine as an anti-inflammatory substance and for the treatment of skin injuries.. This study evaluated the antioxidant activity of methanol (MeOH) and dichloromethane (DC) extracts of five Pittocaulon species.. DC and MeOH extracts from flowers, roots, and stems of Pittocaulon praecox (Cav.) H. Rob. & Brettell, P. bombycophole (Bullock) H. Rob. & Brettell, P. filare (Mc Vaugh) H. Rob. & Brettell, P. velatum (Greenm.) Rob. & Brettell and P. hintonii H. Rob. & Brettell.. In the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, the flower extracts obtained with MeOH were the most active with IC(50) values ranging from 51.83 ± 4.08 to 154.19 ± 8.39 ppm. In the thiobarbituric acid reactive substances (TBARS) model, the best activity was shown by DC extracts of roots with IC(50) values ranging from 55.54 ± 1.28 to 160.82 ± 5.37 ppm. The MeOH extract of flowers of P. bombycophole had the highest IC(50) value in both DPPH (51.83 ± 4.08 ppm) and TBARS (39.78 ± 1.97 ppm). The samples with the best values in the antioxidant activity assays were evaluated in the anti-inflammatory tests. The DC root extract of P. velatum at a dose of 1 mg/ear produced the greatest reduction (84.96%) of the 2-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema. This extract also reduced the activity of the enzyme myeloperoxidase (MPO) (73.65%) at the same dose. In contrast, DC root extract of this species did not show significant inhibition of the increase in paw edema induced by carrageenan at the doses tested (100 mg/kg).. These results support the traditional use of these plants as anti-inflammatory. DC extracts of P. velatum and MeOH extracts of P. bombycophole may be a potential resource of natural anti-inflammatory and antioxidant compounds, respectively. Additional studies must be done to identify the compounds responsible of the activity on these plants and to establish the mechanism of action.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Asteraceae; Biphenyl Compounds; Brain; Carrageenan; Disease Models, Animal; Dose-Response Relationship, Drug; Edema; Enzyme Inhibitors; Flowers; Lipid Peroxidation; Male; Methanol; Methylene Chloride; Mexico; Mice; Peroxidase; Picrates; Plant Extracts; Plant Roots; Plant Stems; Plants, Medicinal; Rats; Rats, Wistar; Solvents; Tetradecanoylphorbol Acetate; Thiobarbituric Acid Reactive Substances

Morus alba Linn. (MA), mulberry leaves have been used as a beverage for prevention of various diseases including hyperlipidemia and hyperglycemia. Recently, the antioxidant activities of the MA leaf extract have been reported. The objective of this study was to investigate the effect of the MA leaf extract on free radical-induced cellular injury. In the in vitro models, the extract scavenged stable free radical (1, 1-diphenyl-2-picrylhydrazyl; DPPH) in a concentration-dependent manner with an IC(50) of 20.10 ± 0.78 μ g/ml. The extract protected the erythrocytes from free radical (2, 2'-azobis (2-amidinopropane) dihydrochloride; AAPH)-induced hemolysis with an IC(50) of 74.22 ± 9.87 μg/ml. Additionally, the extract significantly prevented the gastric mucosal injury induced by ischemia-reperfusion (I/R) in rats when given orally at doses of 0.25 and 0.50 g/kg/day for 3 consecutive days (p < 0.05; n=7). However, this effect was not found when the higher doses (1 and 2 g/kg/day) of the extract were tested. In conclusion, these results indicate that the MA leaf extract possesses the cytoprotective activity against free radical-induced cell injury. Therefore, when given at the appropriate dose range, the mulberry leaf may potentially be used as a food supplement in patients with certain diseases in which the oxidative stress-induced cellular injury is pathologically involved.

Topics: Animals; Antioxidants; Biphenyl Compounds; Cytoprotection; Disease Models, Animal; Dose-Response Relationship, Drug; Erythrocytes; Gastric Mucosa; Hemolysis; Male; Morus; Oxidative Stress; Picrates; Plant Extracts; Plant Leaves; Plants, Medicinal; Rats; Rats, Sprague-Dawley; Reperfusion Injury; Time Factors

Alzheimer's disease (AD) pathogenesis involves an imbalance between free radical formation and destruction. In order to obtain a novel preclinical anti-AD drug candidate, we synthesized a series of novel hydroxyl chalcone analogs which possessed anti-free radical activity, and screened their effects on scavenging 2,2-diphenyl-1-picrylhydrazyl (DPPH) and OH free radicals in vitro. Compound C7, 4,2'-dihydroxy-3,5-dimethoxychalcone was found to have potent activity in these anti-free radical activity tests. Further research revealed that C7 could elevate glutathione peroxidase (GSH-PX) and super oxide dismutase (SOD) levels and lower malonaldehyde (MDA) level in vivo in the Alzheimer's model. The indication of C7's effect on AD needs further study.

Topics: Alzheimer Disease; Animals; Benzophenones; Biphenyl Compounds; Brain; Chalcone; Disease Models, Animal; Free Radical Scavengers; Free Radicals; Glutathione Peroxidase; Hydroxylation; Inhibitory Concentration 50; Magnetic Resonance Spectroscopy; Malondialdehyde; Mice; Oxidation-Reduction; Picrates; Scopolamine; Superoxide Dismutase

The present study was designed to demonstrate the antioxidant and hepatoprotective effect of Majoon-e-Dabeed-ul-ward, a Unani herbal formulation. The Majoon-e-Dabeed-ul-ward (MD) at the doses of 250, 500 and 1000 mg/kg, p.o. was administered after carbon-tetrachloride (CCl(4); 1.5 ml/kg, i.p. once only) intoxication. Treatment with MD at three doses brought the levels of aspartate transaminase, alanine transaminase, albumin and urea in dose dependent manner. Signification reduction was found in TBARS content and restored the level of reduced glutathione, adenosine triphosphatase, and glucose-6-phosphatase in liver. Therapy of MD showed its protective effect on biochemical and histopathological observation at all the three doses in a dose dependent manner. The study conducted showed that MD possesses strong hepatoprotective activity as decrease the hexobarbitone sleep time and improvement in physiological parameter, excretory capacity (BSP retention time) was seen. DPPH and H(2)O(2) scavenging effects indicated its potent antioxidant activities. The results revealed that MD could afford significant dose-dependent protection against CCl(4) induced hepatocellular injury.

Topics: Animals; Antioxidants; Biphenyl Compounds; Carbon Tetrachloride; Chemical and Drug Induced Liver Injury; Disease Models, Animal; Dose-Response Relationship, Drug; Female; Free Radical Scavengers; Hydrogen Peroxide; Lipid Peroxidation; Liver; Liver Function Tests; Medicine, Unani; Mice; Picrates; Plant Preparations; Plants, Medicinal; Rats; Rats, Sprague-Dawley

The leaves of Michauxia species are used for the treatment of wounds in Turkish traditional medicine. In the present study, wound healing, anti-inflammatory and antioxidant activities of the extracts obtained from the root and herb of 5 species of Michauxia collected in different parts of Turkey were evaluated.. In vivo incision and excision wound models were used in order to assess the wound healing effects of the methanolic extracts of the plants. Skin samples were also evaluated histopathologically. In vivo inhibitory effect of the extracts on acetic acid-induced increase in capillary permeability was studied for the assessment of anti-inflammatory activity. TBA (thiobarbituric acid) test, qualitative and quantitative DPPH (2,2-diphenyl-1-picrylhydrazyl) tests were used to evaluate the antioxidant activity.. Noteworthy wound healing activity was observed for the ointment formulation prepared with 1% Michauxia nuda (root) and Michauxia tchihatchewii (herb) extracts. The results of histopathological evaluation supported the outcome of incision and excision wound models. Moreover, the Michauxia nuda (root) exerted remarkable anti-inflammatory effect. The highest antioxidant activity was observed with the ethyl acetate extract of Michauxia tchihatchewii herb.. The experimental study revealed that Michauxia displays remarkable wound healing and anti-inflammatory and antioxidant activities.

Topics: Acetic Acid; Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Campanulaceae; Capillary Permeability; Disease Models, Animal; Dose-Response Relationship, Drug; Inflammation; Lipid Peroxidation; Male; Mice; Picrates; Plant Extracts; Plant Leaves; Plant Roots; Plants, Medicinal; Rats; Rats, Sprague-Dawley; Skin; Thiobarbituric Acid Reactive Substances; Turkey; Wound Healing

The purpose of this study was to investigate the effect of astaxanthin extracted from Paracoccus carotinifaciens on gastric mucosal damage in murine gastric ulcer models. Mice were pretreated with astaxanthin for 1 h before ulcer induction. Gastric ulcers were induced in mice by oral administration of hydrochloride (HCl)/ethanol or acidified aspirin. The effect of astaxanthin on lipid peroxidation in murine stomach homogenates was also evaluated by measuring the level of thiobarbituric acid reactive substance (TBARS). The free radical scavenging activities of astaxanthin were also measured by electron spin resonance (ESR) measurements. Astaxanthin significantly decreased the extent of HCl/ethanol- and acidified aspirin-induced gastric ulcers. Astaxanthin also decreased the level of TBARS. The ESR measurement showed that astaxanthin had radical scavenging activities against the 1,1-diphenyl-2-picrylhydrazyl radical and the superoxide anion radical. These results suggest that astaxanthin has antioxidant properties and exerts a protective effect against ulcer formation in murine models.

Topics: Acids; Animals; Anti-Ulcer Agents; Aspirin; Biphenyl Compounds; Disease Models, Animal; Ethanol; Free Radical Scavengers; Gastric Mucosa; Lipid Peroxidation; Male; Mice; Paracoccus; Picrates; Stomach; Stomach Ulcer; Thiobarbituric Acid Reactive Substances; Xanthophylls

Senecio candicans DC (Asteraceae) is used as a remedy for gastric ulcer and stomach pain in the Nilgiris district, Tamil Nadu for which no scientific evidence exists.. The present study was performed to evaluate the gastroprotective effects and acute oral toxicity of aqueous leaf extract of Senecio candicans (AESC) in experimental models.. The antiulcerogenic activity of AESC was performed in two different ulcer models viz., pylorus-ligated model and ethanol-induced model using Wistar albino rats. Acute toxicity study was also performed to get information on the admissible dose for treatment of ulcer. Preliminary phytochemical screening of AESC was performed to find the active principles present, which are thus responsible for the antiulcerogenic activity. DPPH assay was performed to confirm the antioxidant activity of AESC.. The acute toxicity study did not show any mortality up to 2500mg/kg b.w. of AESC. Both the ulcer models showed gastroprotective effect comparable to that of the standard Omeprazole. The results of antioxidant enzymes, histopathology sections, ATPase and mucus content of gastric secretion showed that several mechanisms are involved in the gastroprotective effect. The preliminary phytochemical screening revealed the presence of alkaloids, flavonoids and steroids in AESC. The DPPH assay confirmed the antioxidant activity of AESC.. The traditional consumption of AESC for the treatment of gastric ulcer is thus true, the antioxidant constituents present in the extract plays a major role in the gastroprotective activity, but since Senecio species are known for the presence of pyrrolizidine alkaloids, a detailed study in future is required to describe the safe dose for a prolonged period.

Topics: Adenosine Triphosphatases; Alkaloids; Animals; Anti-Ulcer Agents; Antioxidants; Biphenyl Compounds; Disease Models, Animal; Female; Flavonoids; Gastric Juice; Gastric Mucosa; India; Male; Mucus; Omeprazole; Picrates; Plant Extracts; Plant Leaves; Rats; Rats, Wistar; Senecio; Steroids; Stomach; Stomach Ulcer

Meconopsis quintuplinervia, a medicinal herb endemic to the Tibetan region, is used to treat hepatitis. The aim of this study is to evaluate the antioxidant potential of the ethanolic extract of this herb using different assays.. The antioxidant capacity of Meconopsis quintuplinervia was investigated using various established in vitro systems. An in vivo study of carbon tetrachloride (CCl(4))-induced antioxidant activity in mice was also conducted by examining the levels of malondialdehyde (MDA) and the activities of antioxidant enzymes, including superoxide dismutase (SOD), catalase (CAT), and glutathione (GSH).. The extract showed strong in vitro antioxidant ability. In the in vivo study, CCl(4)-induced oxidative stress caused significant decreases in the SOD, CAT, and GSH levels and a significant increase in the MDA level, most of which were significantly reversed (except for SOD in the liver.) by treatment with the extract and standard Vitamin E.. This study clearly indicates that the ethanolic extract of Meconopsis quintuplinervia is a valuable source of natural antioxidants. These findings provide scientific support for the traditional use of this herb as a Tibetan medicine for liver diseases.

Topics: Animals; Antioxidants; Benzothiazoles; Biphenyl Compounds; Carbon Tetrachloride; Catalase; Chelating Agents; Chemical and Drug Induced Liver Injury; Disease Models, Animal; Dose-Response Relationship, Drug; Ethanol; Female; Flavonoids; Glutathione; Lipid Peroxidation; Liver; Male; Malondialdehyde; Mice; Oxidation-Reduction; Oxidative Stress; Papaveraceae; Phenols; Phytotherapy; Picrates; Plant Extracts; Plants, Medicinal; Rats; Rats, Sprague-Dawley; Solvents; Sulfonic Acids; Superoxide Dismutase; Vitamin E

Cyathula prostrata (Linn) Blume (Amaranthaceae) is an annual herb widely used traditionally in the treatment of various inflammatory and pain related health disorders in Nigeria. The aim of this study is to evaluate the anti-inflammatory, analgesic and antioxidant activities of the methanolic extract of Cyathula prostrata (Linn) Blume.. The anti-inflammatory (phorbol 12-myristate 13-acetate (PMA)-induced reactive oxygen species (ROS), lipopolysaccharide (LPS) induced nitric oxide production in U937 macrophages, LPS-induced COX-2 expression, carrageenan-induced rat paw oedema, arachidonic acid-induced ear oedema and xylene-induced ear oedema), analgesic (acetic acid-induced writhing and hot plate tests) and antioxidant activities (DPPH [1,1-diphenyl-2-picrylhydrazyl] and lipid peroxidation assays) activities of the plant extract were investigated.. The methanolic extract of Cyathula prostrata did not show inhibitory activity in the in vitro PMA-induced reactive oxygen species, LPS-induced nitric oxide production and LPS-induced COX-2 expression assays. In the in vivo anti-inflammatory assays, the extract (50, 100 and 200mg/kg) showed a significant (P<0.05) dose-dependent inhibition in the carrageenan, arachidonic acid and xylene-induced tests. Cyathula prostrata produced a significant (P<0.05, 0.001) dose-dependent inhibition in the acetic acid and hot plate analgesic tests respectively. The plant extract did not exhibit any antioxidant activity in the DPPH and lipid peroxidation assays.. The results suggest that the methanolic extract of Cyathula prostrata possesses anti-inflammatory and analgesic activities and this authenticates the use of the plant in the traditional treatment of ailments associated with inflammation and pain.

Topics: Acetic Acid; Amaranthaceae; Analgesics; Animals; Anti-Inflammatory Agents; Antioxidants; Arachidonic Acid; Behavior, Animal; Biphenyl Compounds; Carrageenan; Cyclooxygenase 2; Disease Models, Animal; Dose-Response Relationship, Drug; Female; Hot Temperature; Humans; Inflammation; Inflammation Mediators; Lipid Peroxidation; Lipopolysaccharides; Macrophages; Male; Methanol; Mice; Motor Activity; Nitric Oxide; Oxidative Stress; Pain; Pain Threshold; Phytotherapy; Picrates; Plant Preparations; Plants, Medicinal; Rats; Rats, Wistar; Reactive Oxygen Species; Solvents; Tetradecanoylphorbol Acetate; U937 Cells; Xylenes

Herbal medicines have traditionally been used worldwide for the prevention and treatment of liver disease with fewer adverse effects. The leaves of the Syzygium jambos (SJL) plant were chosen and studied for their antioxidant activity in vitro and hepatoprotective activity in vivo. The antioxidant activity of the ethanol extract was examined in vitro using a 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay, reducing capacity, total phenol, total flavonoid content, and total antioxidant capacity. The extract had significant dose-dependent antioxidant activity in all in vitro experiments. IC(50) values of SJL and ascorbic acid (standard) were found to be 14.10 and 4.87 μg/mL, respectively, according to a DPPH radical scavenging assay. Hepatoprotective activity of the plant extract was evaluated in a rat model of carbon tetrachloride (CCl(4))-induced liver damage. CCl(4) significantly altered serum marker enzymes, total bilirubin, total protein, and liver weight. The extract caused these values to return to normal in rats with CCl(4)-induced liver damage that were given SJL. This indicated the hepatoprotective potential of SJL and was comparable to use of the standard drug silymarin. Thus, the present study revealed that SJL may have antioxidant and hepatoprotective activity.

Topics: Animals; Antioxidants; Biomarkers; Biphenyl Compounds; Carbon Tetrachloride; Chemical and Drug Induced Liver Injury; Disease Models, Animal; Dose-Response Relationship, Drug; Ethanol; Liver; Picrates; Plant Extracts; Plant Leaves; Rats; Syzygium

The antioxidant activities of the crude hydro-alcoholic extract (CE) and its four fractions viz. methanol (MF), ethyl acetate (EF), n-Butanol (BF), and precipitated aqueous (PAF) of A.racemosus roots tested decreased in the order of EF > MF > CE > BF > PAF when investigated by DPPH free radical scavenging assay. Under iron induced lipid peroxidation almost similar results were observed except that the activity was more in PAF than BF. Hepatoprotective activity of the extracts was also demonstrable in vivo by the inhibition of-CCl4 induced formation of lipid peroxides in the liver of rats by pretreatment with the extracts. CCl4-induced hepatotoxicity in rats, as judged by the raised serum enzymes viz. glutamate oxaloacetate transaminase, glutamate pyruvate transaminase, alkaline phosphatase and total and direct bilirubin as well as oxidant enzyme viz. malon dialdehyde were prevented, while antioxidant enzymes viz. superoxide dismutase, reduced glutathione and catalase were elevated by pretreatment with the extracts, demonstrating the potent hepatoprotective action of the roots of A. racemosus.

Topics: Animals; Antioxidants; Asparagus Plant; Biphenyl Compounds; Carbon Tetrachloride; Chemical and Drug Induced Liver Injury; Disease Models, Animal; Lipid Peroxidation; Liver; Liver Function Tests; Male; Picrates; Plant Extracts; Plant Roots; Rats; Rats, Wistar

We made an attempt to evaluate the preventive effects of vanillic acid on isoproterenol-induced myocardial infarcted rats. Rats were pretreated with vanillic acid (5 and 10 mg/kg) daily for 10 days. After pretreatment, rats were injected with isoproterenol (100 mg/kg) at an interval of 24 h for 2 days to induce myocardial infarction. Isoproterenol induction increased the activity of serum creatine kinase-MB and increased the levels of serum and heart cholesterol, triglycerides, free fatty acids in rats. It increased the levels of serum low density and very low density lipoprotein cholesterol and decreased the levels of high-density lipoprotein cholesterol. Also, the activity of 3-hydroxy-3methyl glutaryl-coenzyme-A-reductase in the plasma and liver was increased, and lecithin cholesterol acyl transferase activity in the plasma and liver was decreased in isoproterenol-induced rats. Furthermore, isoproterenol-induced rats showed a decrease in myocardial expression of B-cell leukemia/lymphoma-2(bcl-2) gene and an increase in myocardial expression of bcl-2 associated-x (bax)-gene. Vanillic acid pretreated isoproterenol-induced rats positively altered all the above-mentioned biochemical parameters. Vanillic acid pretreatment also reduced myocardial infarct size in myocardial infarcted rats. In vitro study confirmed the potent free radical scavenging effect of vanillic acid. The observed effects are due to free radical scavenging effects of vanillic acid. This study may have a significant impact on myocardial infarcted patients.

Topics: Animals; bcl-2-Associated X Protein; Biphenyl Compounds; Creatine Kinase, MB Form; Disease Models, Animal; Free Radical Scavengers; Gene Expression Regulation; Isoproterenol; Lipid Metabolism; Lipids; Male; Myocardial Infarction; Myocardium; Picrates; Proto-Oncogene Proteins c-bcl-2; Rats; Rats, Wistar; Vanillic Acid

The antioxidant and drug metabolizing potentials of Hibiscus anthocyanin extract in CCl(4)- induced oxidative damage of rat liver was investigated. Hibiscus anthocyanin extract effectively scavenge α-diphenyl-β-picrylhydrazyl (DPPH) radical, superoxide ion, and hydrogen peroxide. It produced a 92% scavenging effect of DPPH radical at a concentration of 2.0 mg/mL. Hibiscus anthocyanin extract produced a 69 and 90% scavenging effect on superoxide ion and hydrogen peroxide, respectively, at 1.0 mg/mL, which compared favorably with the synthetic antioxidant (butylated hydroanisole and α-tocopherol). A reducing power of this anthocyanin was examined using K(3)Fe(CN)(6). Hibiscus anthocyanin extract has reducing power that is approximately 2-fold that of the synthetic antioxidant, butylated hydroanisole. Hibiscus anthocyanin extract produced a significantly increase and completely attenuated the CCl(4)-mediated decrease in antioxidant enzymes (e.g., catalase, superoxide dismutase, glutathione peroxidase, and glutathione reductase). However, the level of nonenzymic antioxidant molecules (i.e., vitamins C and E) were significant preserved by Hibiscus anthocyanin extract. There was an induction of phase II drug-detoxifying enzymes: glutathione S-transferase, NAD(H):quinone oxidoreductase, and uridyl diphosphoglucuronosyl transferase by 65, 45, and 57%, respectively. In view of these properties, Hibiscus sabdariffa anthocyanin extract can act as a prophylactic by intervening as a free radical scavenger both in vitro and in vivo as well as inducing the phase II drug detoxification enzymes.

Topics: Animals; Anthocyanins; Biphenyl Compounds; Chemical and Drug Induced Liver Injury; Disease Models, Animal; Enzyme Induction; Free Radical Scavengers; Free Radicals; Hibiscus; In Vitro Techniques; Inactivation, Metabolic; Lipid Peroxidation; Liver; Male; Oxidative Stress; Oxidoreductases; Picrates; Plant Extracts; Rats

Salvia L. species are widely used against wounds and skin infections in Turkish folk medicine.. The aim of the present study is to evaluate wound healing activity of the ethanol (EtOH) extracts of Salvia cryptantha and Salvia cyanescens.. For the assessment of wound healing activity linear incision and circular excision wound models were employed on rats and mice. The wound healing effect was comparatively evaluated with the standard skin ointment Madecassol(®). Inhibition of tyrosinase, a key enzyme in skin aging, was achieved using ELISA microplate reader. Antioxidant activity was evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide radical scavenger effect, ferrous ion-chelating ability, and ferric-reducing antioxidant power (FRAP) tests.. The EtOH extract of Salvia cryptantha treated groups of animals showed 56.5% contraction, whereas the reference drug Madecassol(®) showed 100% contraction. On the other hand, the same extract on linear incision wound model demonstrated a significant increase (33.2%) in wound tensile strength as compared to other groups. The results of histopathological examination maintained the upshot of linear incision and circular excision wound models as well. These findings specify that Salvia cryptantha for wound healing activity can be appealed further phytochemical estimation for spotting its active components.

Topics: Animals; Anti-Infective Agents; Antioxidants; Biphenyl Compounds; Disease Models, Animal; Male; Medicine, Traditional; Mice; Monophenol Monooxygenase; Phytotherapy; Picrates; Plant Components, Aerial; Plant Extracts; Rats; Rats, Sprague-Dawley; Salvia; Skin; Tensile Strength; Triterpenes; Turkey; Wound Healing; Wounds, Stab

Boesenbergia rotunda (L) Mansf. has been used for the treatment of gastrointestinal disorders including peptic ulcer. In the current study we aimed to investiagte the anti-ulcer activities of methanolic extract of B. rotunda (MEBR) and its main active compound, pinostrobin on ethanol-induced ulcer in rats. The possible involevement of lipid peroxidation, nitric oxide, cyclooxygenases and free radical scavenging mechanisms also has been investigated.. Pinostrobin was isolated form the rhizomes of B. rotunda. Ulcer index, gastric juice acidity, mucus content, gross and histological gastric lesions and thiobarbituric acid reactive substances (TBARS) were evaluated in ethanol-induced ulcer in vivo. The effect of pinostrobin into lipopolysaccharide/interferon-γ stimulated rodent cells, COX-1 and COX-2 activities were done in vitro.. Pre-treatment with MEBR, pinostrobin or omeprazole protected the gastric mucosa as seen by reduction in ulcer area and mucosal content, reduced or absence of submucosal edema and leucocytes infiltration. Pinostrobin significantly (p<0.05) lowered the elevated TBARS level into gasteric homogenate. Pinostrobin did not produced significant in vitro inhibition of NO from LPS/IFN-γ activated rodent cells without affecting the viability of these cells. Further, the compound did bot revleaed inhibitory effects on both COX- 1& 2 enzymes. The antioxidant assays also exhibited non significance in vitro.. Thus it can be concluded that MEBR possesses anti-ulcer activity, which could be attributed to indirect anti-oxidant mechanism of pinostrobin but not to the intervention with nitric oxide and COX inflammation pathways.

Topics: Animals; Anti-Ulcer Agents; Antioxidants; Biphenyl Compounds; Cell Line; Cell Survival; Chemotaxis, Leukocyte; Cyclooxygenase 1; Cyclooxygenase 2; Disease Models, Animal; Ethanol; Female; Flavanones; Free Radicals; Gastric Mucosa; Macrophages; Male; Methanol; Mice; Picrates; Plant Extracts; Rats; Rats, Sprague-Dawley; Rhizome; Stomach Ulcer; Toxicity Tests, Acute; Zingiberaceae

[corrected] The Taxillus liquidambaricola has been used to treat rheumatic arthralgia, threatened abortion and hypertension in the Chinese traditional medicine. However, there is no scientific evidence which supports the use in the literature. This study aimed to determine the antioxidant, and analgesic activities and the mechanism of anti-inflammatory activities of the ethanolic extracts of Taxillus liquidambaricola (ETL) in cell and animal models.. The following activities were investigated: free radical scavenging and antioxidant activities [2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), and DPPH (1, 1-diphenyl-2-picrylhydrazyl)], analgesic (writhing and formalin test), and anti-inflammatory [lipopolysaccharide (LPS) induced nitric oxide (NO) production in RAW264.7 macrophages and paw-edema induced by λ-carrageenan (Carr)]. We also investigate the anti-inflammatory mechanism of ETL via studies of the activities of catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPx) and the levels of malondialdehyde (MDA) in the edema paw. Serum NO and tumor necrosis factor α (TNF-α) were also measured in vivo.. ETL showed the highest TEAC and DPPH radical scavenging activities, respectively. ETL also had highest contents of polyphenol and flavonoid contents. We evaluated that ETL and the reference compound of quercetin decreased the LPS-induced NO production and expressions of iNOS and COX-2 in RAW264.7 cells. Treatment of male ICR mice with ETL significantly inhibited the numbers of acetic acid-induced writhing response and the formalin-induced pain in the late phase. Administration of ETL showed a concentration dependent inhibition on paw edema development after Carr treatment in mice. The anti-inflammatory effects of ETL could be via NO and TNF-α suppression and associated with the increase in the activities of antioxidant enzymes. Western blotting revealed that ETL decreased Carr-induced inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) expressions.. Anti-inflammatory mechanisms of ETL might be correlated to the decrease in the level of MDA, iNOS, and COX-2 via increasing the activities of CAT, SOD, and GPx in the edema paw. Overall, the results showed that ETL demonstrated antioxidant, antinociceptive, and anti-inflammatory activity, which supports previous claims of the traditional use for inflammation and pain.

Topics: Acetic Acid; Analgesics; Animals; Anti-Inflammatory Agents; Antioxidants; Benzothiazoles; Biphenyl Compounds; Carrageenan; Catalase; Cell Line; Chromatography, High Pressure Liquid; Cyclooxygenase 2; Disease Models, Animal; Dose-Response Relationship, Drug; Drugs, Chinese Herbal; Edema; Endotoxins; Ethanol; Formaldehyde; Glutathione Peroxidase; Loranthaceae; Macrophages; Male; Malondialdehyde; Mice; Mice, Inbred ICR; Nitric Oxide; Nitric Oxide Synthase Type II; Pain; Picrates; Plants, Medicinal; Solvents; Sulfonic Acids; Superoxide Dismutase; Thiazoles; Time Factors; Tumor Necrosis Factor-alpha

Phyllanthus simplex (Family: Euphorbiacae) is widely used in traditional medicines for treatment of various diseases including inflammation.. Petroleum ether extract (PSPE) and ethanol extract (PSEE) of the whole plant of Phyllanthus simplex were characterized for their total phenolics, tannins and flavonoids content. These extracts were standardized by HPTLC using phyllanthin and gallic acid respectively as markers. Antioxidant activity of extracts was evaluated by the DPPH, hydroxyl and superoxide radicals scavenging assay. The total antioxidant capacity of extracts was determined. Anti-inflammatory activity was evaluated by their effect on nitric oxide (NO) production in isolated rat peritoneal macrophages; carragennan-induced paw edema and formation of cotton pellet-induced granuloma in rats.. Abundance of phenolics was found in PSEE. Phyllanthin and gallic acid content in PSPE and PSEE were found to be 14.5 and 0.65% (w/w) respectively. PSEE showed concentration dependent significant scavenging of DPPH, hydroxyl and superoxide radicals with IC(50) values 102.219, 171.485 and 24.73 μg/ml respectively. PSEE significantly inhibited NO production in isolated rat peritoneum macrophages. Moreover, it also exhibited significant inhibition of carragennan-induced paw edema (58.48 ± 0.028%, p < 0.001, at 6h, 200 mg/kg oral dose) and cotton pellet-induced granuloma formation (45.671 ± 0.712%, p < 0.001, at 200mg/kg oral dose). Anti-inflammatory activity of PSEE was found to be comparable to diclofenac sodium.. Significant antioxidant and anti-inflammatory activities were found in PSEE which may be attributed to its high phenolic content.

Topics: Alkanes; Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Carrageenan; Cells, Cultured; Chromatography, High Pressure Liquid; Cotton Fiber; Disease Models, Animal; Dose-Response Relationship, Drug; Edema; Ethanol; Female; Flavonoids; Granuloma, Foreign-Body; Hydroxyl Radical; Macrophages, Peritoneal; Male; Nitric Oxide; Phenols; Phyllanthus; Picrates; Plant Extracts; Plants, Medicinal; Rats; Rats, Wistar; Solvents; Superoxides; Tannins

Solar ultraviolet radiation (UV) is a major cause of non-melanoma skin cancer in humans. Photochemoprevention with natural products represents a simple but very effective strategy in the management of cutaneous neoplasia. The study investigated the protective activity of Calluna vulgaris (Cv) and red grape seeds (Vitis vinifera L, Burgund Mare variety) (BM) extracts in vivo on UVB-induced deleterious effects in SKH-1 mice skin. Forty SKH-1 mice were randomly divided into 4 groups (n=10): control, UVB irradiated, Cv + UVB irradiated, BM+UVB irradiated. Both extracts were applied topically on the skin in a dose of 4 mg/40 μl/cm(2) before UVB exposure - single dose. The effects were evaluated in skin 24 hours after irradiation through the presence of cyclobutane pyrimidine dimers (CPDs) and sunburn cells, tumor necrosis factor-alpha (TNF-α), interleukin (IL)-6 levels. The antioxidant activity of BM extract was higher than those of Cv extract as determined using stable free radical DPPH assay and ABTS test. One single dose of UVB generated formation of CPDs (p<0.0001) and sunburn cells (p<0.0002) and increased the cytokine levels in skin (p<0.0001). Twenty hours following irradiation BM extract inhibited UVB-induced sunburn cells (p<0.02) and CPDs formation (p<0.0001). Pretreatment with Cv and BM extracts resulted in significantly reduced levels of IL-6 and TNF-α compared with UVB alone (p<0.0001). Our results suggest that BM extracts might be a potential candidate in preventing the damages induced by UV in skin.

Topics: Animals; Apoptosis; Biphenyl Compounds; Calluna; Cytokines; Disease Models, Animal; Female; Free Radical Scavengers; Humans; Mice; Mice, Hairless; Phytotherapy; Picrates; Plant Extracts; Pyrimidine Dimers; Random Allocation; Seeds; Skin; Skin Neoplasms; Sunburn; Ultraviolet Rays; Vitis

Ischemia/reperfusion (I/R) injury is characterized by significant oxidative stress, which induces characteristic changes in the antioxidant system and organ injury leading to significant morbidity and mortality. The aim of this study was to evaluate the protective effect of dihydrolipoyl histidinate zinc complex (DHLHZn) on oxidative damage after severe hepatic I/R injury.. Thirty male Wistar rats were subjected to 45 min of hepatic ischemia by clamping of the hepatic artery and portal vein, followed by a 6-h reperfusion period. DHLHZn (10 mg/kg) (I/R + DHLHZn group) or saline (I/R group) was administered intraperitoneally twice, 30 min before ischemia and at the beginning of the reperfusion. Sham-operated animals (sham group) received equal amounts of saline. The rats were killed at the end of the reperfusion period. Serum levels of aspartate aminotransferase and alanine aminotransferase were determined, and histological examination and oxidative stress were evaluated in liver tissues. In addition, antimycin A-stimulated RAW264.7 cells (murine macrophage-like cells) were treated with DHLHZn to estimate its antioxidant effect.. Serum aspartate aminotransferase and alanine aminotransferase levels were increased in the I/R group, but these increases were significantly inhibited in the I/R + DHLHZn group. Similarly, liver tissue damage observed in the I/R group was attenuated in the I/R + DHLHZn group. Cells treated in vitro with both DHLHZn and antimycin A showed reduced reactive oxygen species activity compared to cells treated with antimycin A alone.. The new antioxidant DHLHZn may have potential for therapeutic application in liver I/R injury, although this is a limited animal study.

Topics: Alanine Transaminase; Animals; Antimycin A; Antioxidants; Aspartate Aminotransferases; Biomarkers; Biphenyl Compounds; Cell Line; Disease Models, Animal; Dose-Response Relationship, Drug; Histidine; Liver; Liver Diseases; Male; Malondialdehyde; Mice; Oxidative Stress; Picrates; Rats; Rats, Wistar; Reactive Oxygen Species; Reperfusion Injury; Thioctic Acid; Time Factors

Antioxidant and gastroprotective activities of aqueous and ethanolic extract of Andrographis paniculata leaves in rats have been reported. Sprague Dawley rats, 6 per group were used and rats in groups 1 to 6 were pretreated with (0.25% w/v) carboxymethyl cellulose (negative control, 5 ml/kg), 20 mg/kg omeprazole (positive control), (250 mg/kg and 500 mg/kg) of aqueous leaf extracts (APLAE) and (250 and 500 mg/kg) of ethanol leaf extracts (APLEE) respectively. Animals were orally administered with 95% ethanol (5 ml/kg) 60 min after their pretreatments. Rats were sacrificed 1 h after treatment and gastric contents were collected to measure pH and mucous weight. Stomach was analyzed for gross and histological changes. Ulcer control group showed extensive lesions of gastric mucosal layer, whereas rats pretreated with omeprazole, 250 and 500 mg/kg of APLAE showed significant and dose dependent reduction in gastric lesions with increased pH and mucus content of stomach. Rats pretreated with 250 or 500 mg/kg of APLEE showed significantly better inhibition of gastric mucosal lesions. Further, the in vitro antioxidant studies using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay showed that ethanol extracts have superior free radical scavenging activity with IC50 value = 10.9 than aqueous extracts with IC50 value = 24.65. Results of this study showed that pretreatment with ethonolic extract of A. paniculata ethanolic provided significant protection against gastric ulcer by regulating of pH, mucous production and antioxidant property.

Topics: Andrographis; Animals; Anti-Ulcer Agents; Biphenyl Compounds; Disease Models, Animal; Ethanol; Free Radical Scavengers; Free Radicals; Gastric Mucosa; Male; Picrates; Plant Extracts; Plant Leaves; Rats; Rats, Sprague-Dawley; Stomach Ulcer; Water

To investigate protective effects of Marrubium cordatum extract on ovary torsion-detorsion.. Controlled research study.. Marrubium cordatum extract was obtained by methanol extraction.. Six-month-old female New Zealand rabbits.. In the first phase, antioxidant activity of M. cordatum extract was evaluated. In the second phase, M. cordatum extract at doses of 0, 250, 500, and 1,000 mg/kg was studied for dose determination. In the third phase, the protective role of M. cordatum on ovarian torsion-detorsion injury was evaluated in sham control, torsion-detorsion, torsion-detorsion +M. cordatum (1,000 mg/kg).. 1,1-Diphenyl-2-picrylhydrazyl, nitric oxide radical scavenging activity, reducing power capacity, and total phenolic compounds were assayed. Glutathione, malondialdehyde, catalase, and glutathione peroxidase were measured. Histopathological examination was also conducted.. Marrubium cordatum significantly inhibited 1,1-diphenyl-2-picrylhydrazyl, nitric oxide radicals, and showed a powerful reducing activity. Marrubium cordatum did not adversely affect biochemical and histopathological parameters at all doses. Malondialdehyde level and catalase activity in the torsion-detorsion group were significantly increased compared with those of the sham group, whereas the glutathione level and glutathione peroxidase activity were significantly decreased compared with those of the sham group. Marrubium cordatum treatment significantly lowered the malondialdehyde level and catalase activity but increased the glutathione level in torsion-detorsion injury. Histopathologically, severe congestion, hemorrhage, edema, and leukocyte infiltration were observed in the torsion-detorsion group. Marrubium cordatum treatment ameliorated these alterations.. Marrubium cordatum attenuates ischemia-reperfusion-induced biochemical and histopathological alterations.

Topics: Animals; Antioxidants; Biphenyl Compounds; Catalase; Disease Models, Animal; Dose-Response Relationship, Drug; Female; Glutathione; Glutathione Peroxidase; Kidney; Lipid Peroxidation; Liver; Malondialdehyde; Marrubium; Nitric Oxide; Ovarian Diseases; Ovary; Phenols; Picrates; Plant Extracts; Plant Leaves; Rabbits; Reperfusion Injury; Torsion Abnormality

A series of novel conjugates of aspirin with natural phenolic acid antioxidants connected through a diol linker were designed and synthesized as potential bifunctional agents combining antioxidant and anti-inflammatory activity for reducing gastrointestinal toxicity. In general, the conjugates were found to be efficient antioxidants and many of them demonstrated much more potent anti-inflammatory activity than aspirin. Among them, 5a and 5b which bear the best anti-inflammatory activity exhibited significantly reduced ulcerogenic potency and toxicity compared to aspirin. However, it is evident that the anti-inflammatory activity of these dual-acting molecules in vivo, was not simply consistent with their antioxidant ability in vitro.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Aspirin; Biphenyl Compounds; Croton Oil; Disease Models, Animal; Drug Design; Hydroxybenzoates; Inflammation; Lipid Peroxidation; Male; Mice; Molecular Structure; Picrates; Stomach Ulcer; Structure-Activity Relationship

The present study investigated the antinociceptive, anti-inflammatory and antioxidant effects of the leaf essential oil (LEO) of Cymbopogon winterianus Jowitt (Poaceae). In the acetic acid-induced writhing and formalin tests, the LEO (50, 100, and 200 mg/kg, p.o.) significantly reduced (p < 0.05) the number of writhings and paw licking times in the first (0-5 min) and second (15-30 min) phases, respectively. In contrast, the LEO did not alter the latency time for mice licking the rear paws in hot-plate test. The LEO inhibited the carrageenan-induced neutrophil migration to the peritoneal cavity in a dose-dependent manner (35.5%, 42.8%, and 66.1% at doses of 50, 100, and 200 mg/kg, respectively, p < 0.001). Moreover, LEO exhibited higher scavenging activity toward 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals with an IC(50) (12.66 ± 0.56 μg/mL). Our present results demonstrated that the LEO has antinociceptive, anti-inflammatory, and antioxidant properties.

Topics: Acetic Acid; Analgesics; Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Carrageenan; Cymbopogon; Disease Models, Animal; Dose-Response Relationship, Drug; Edema; Hot Temperature; Male; Mice; Oils, Volatile; Pain; Pain Measurement; Phytotherapy; Picrates; Plant Leaves; Plant Oils; Rats; Rats, Wistar

Oxidative stress induced by overproduction of reactive oxygen species (ROS) plays an important role in hypoxia/reoxygenation (H/R) injury. In the present study, effects of salvianolic acid A (1) on heart H/R injury through its antioxidant activity were examined, using a molecule-based ROS scavenging system and cardiomyocyte model of H/R injury, as well as isolated rat heart model. As a result, 1 showed a potent antioxidant activity, scavenging all of the tested ROS and DPPH (2,2-diphenyl-1-picrylhydrazyl). The antioxidant effect of 1 was also observed in cardiomyocytes exposed to H/R. Compound 1 remarkably decreased dihydroethidium and dichlorofluorescein fluorescence and increased cell viability and mitochondrial membrane potential, ΔΨ(m), when compared to the H/R group. In isolated rat hearts exposed to H/R, 1 markedly increased the coronary flow, the peak of pressure development and the valley of pressure development, and significantly reduced the left ventricular end diastolic pressure when compared to the H/R group. These results suggested that 1 had significant protective effects against H/R-induced myocardial injury through its antioxidant activity.

Topics: Animals; Biphenyl Compounds; Caffeic Acids; Cardiotonic Agents; Disease Models, Animal; Heart; Hypoxia; Lactates; Molecular Structure; Myocytes, Cardiac; Oxidative Stress; Picrates; Rats; Reactive Oxygen Species

Pistacia lentiscus has traditionally been used in the treatment of many diseases. Its resin was investigated for its mineral contents, anti-inflammatory and antioxidant activities in rats.. Inhibition of carrageenan induced edema was used to evaluate anti-inflammatory activity. Fe2+ chelating ability, 1,1-diphenyl-2-picryl hydrazyl radical (DPPH) and nitric oxide scavenging activities were used to evaluate antioxidant activities and mineral contents were determined by atomic absorption spectroscopy. Gallic acid content was determined by HPLC.. Resin produced statistically significant inhibition of edema at all doses when compared to the control groups. A 100% inhibition of inflammation was observed at 800 mg/kg i.p. Resin exhibit no toxicity up to 3 g/kg body weights i.p. in mice. Weak DPPH and nitric oxide scavenging activities were observed but showed good Fe2+ chelating ability (IC50 = 162 microg ml(-1)). The amount of elements was decreased in the order: Cu > Fe, Zn > Mn > Ni, Cd. Gallic acid content was 0.1 mg/g resin.. These experimental data support the use of Pistacia lentiscus resin as an antiinflammatory and antioxidant agent.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Carrageenan; Chromatography, High Pressure Liquid; Disease Models, Animal; Dose-Response Relationship, Drug; Edema; Ferrous Compounds; Ferrozine; Flavonoids; Free Radical Scavengers; Gallic Acid; Inflammation; Iron Chelating Agents; Male; Mastic Resin; Mice; Nitric Oxide; Picrates; Rats; Rats, Wistar; Resins, Plant; Spectrophotometry, Atomic

The chromatographic separation of MeOH extract from Clerodendron trichotomum Thunberg leaves led to the isolation of three phenylpropanoid compounds. Using spectroscopic methods, the structures of these compounds were determined as beta-(3', 4'-dihydroxyphenyl)ethyl-O-alpha-L-rhamnopyranosyl (1-->3)-beta-D-(4-O-caffeoyl)-glucopyranoside, acteoside (verbascoside) (1), beta-(3', 4'-dihydroxyphenyl)ethyl-O-alpha-L-rhamnopyranosyl (1-->3)-beta-D-(6-O-caffeoyl)-glucopyranoside, isoacteoside (2), beta-(3', 4'-dihydroxyphenyl) ethyl-O-alpha-L-rhamnopyranosyl (1-->3)-beta-D-glucopyranoside, and decaffeoylacteoside (3). We measured the anti-inflammatory activity of these three phenylpropanoid compounds both in vitro (DPPH reduction assay, TBARS assay on Cu (2+)-induced oxidized LDL, PGE(2) assay) and in vivo (acetic acid induced vascular permeability in mice and carrageenan-induced hind paw edema in rats). 80% methanol fraction and acteoside had the activity.

Topics: Acetic Acid; Animals; Anti-Inflammatory Agents; Biphenyl Compounds; Capillary Permeability; Carrageenan; Catechols; Cell Line; Clerodendrum; Dinoprostone; Disaccharides; Disease Models, Animal; Dose-Response Relationship, Drug; Free Radical Scavengers; Glucosides; Humans; Inflammation; Magnetic Resonance Spectroscopy; Mast Cells; Mice; Molecular Structure; Phenols; Picrates; Plant Leaves; Rats; Thiobarbituric Acid Reactive Substances

Saponins are valuable principles found in various herbal medicine with pharmaceutical, cosmetical and nutraceutical merits. In this study, we evaluated the protective role of saponin fraction (Cl-SF), prepared from Codonopsis lanceolata, an ethnopharmacologically famous plant in Korea, China and Japan, on water immersion stress-induced liver damage and radical generation. Cl-SF clearly decreased the up-regulated levels of serum glutamate-oxalacetate transaminase and glutamate-pyruvate-transaminase induced by water-immersed stress conditions. Furthermore, Cl-SF seemed to block the stress-induced radicals. Thus, Griess and DPPH assays revealed that Cl-SF significantly suppressed both radical generation in sodium nitroprusside-treated RAW264.7 cells and nitric oxide production in LPS-treated RAW264.7 cells. Therefore, these results suggest that Cl-SF may be considered as a promising stress-regulatory principle with radical scavenging actions.

Topics: Animals; Biphenyl Compounds; Cell Line; Cell Proliferation; Cell Survival; Codonopsis; Disease Models, Animal; Free Radical Scavengers; Immersion; Liver Diseases; Male; Mice; Mice, Inbred ICR; Nitric Oxide; Picrates; Reactive Oxygen Species; Saponins; Stress, Psychological

An emulsion system composed of vitamin E, coconut oil, soybean phosphatidylcholine, non-ionic surfactants, and polyethylene glycol (PEG) derivatives (referred to as the tocol emulsion) was characterized in terms of its physicochemical properties, drug release, in vivo efficacy, toxicity, and stability. Systems without vitamin E (referred to as the lipid emulsion) and without any oils (referred to as the aqueous micelle system) were prepared for comparison. A lipophilic antioxidant, resveratrol, was used as the model drug for emulsion loading. The incorporation of Brij 35 and PEG derivatives reduced the vesicle diameter to <100nm. The inclusion of resveratrol into the emulsions and aqueous micelles retarded the drug release. The in vitro release rate showed a decrease in the order of aqueous micelle system>tocol emulsion>lipid emulsion. Treatment of resveratrol dramatically reduced the intimal hyperplasia of the injured vascular wall in rats. There was no significant difference in this reduction when resveratrol was delivered by either emulsion or the aqueous micelle system. The percentages of erythrocyte hemolysis by the emulsions and aqueous micelle system were approximately 0 and approximately 10%, respectively. Vitamin E prevented the aggregation of emulsion vesicles. The mean vesicle size of the tocol emulsion remained unchanged during 30 days at 37 degrees C. The lipid emulsion and aqueous micelle system, respectively, showed 11- and 16-fold increases in vesicle size after 30 days of storage.

Topics: Animals; Antioxidants; Biphenyl Compounds; Carotid Stenosis; Chemistry, Pharmaceutical; Coconut Oil; Disease Models, Animal; Drug Carriers; Drug Compounding; Emulsions; Hemolysis; Male; Micelles; Oils; Particle Size; Phosphatidylcholines; Picrates; Plant Oils; Polyethylene Glycols; Rats; Rats, Sprague-Dawley; Resveratrol; Solubility; Stilbenes; Surface-Active Agents; Technology, Pharmaceutical; Time Factors; Vitamin E

The preventive effect of Anemarrhena asphodeloides Bunge (Liliaceae), a traditional Chinese medicine, on ischemia-reperfusion-induced brain injury was evaluated in the rat brain. Ischemia was induced by intraluminal occlusion of the right middle cerebral artery for 2 h and reperfusion was continued for 22 h. Water extract of Anemarrhena asphodeloides (WEAA) was orally administered promptly prior to and 2 h after reperfusion. Total infarct volume and edema in the ipsilateral hemispheres of ischemia-reperfusion rats were significantly reduced by treatment with WEAA in a dose-dependent manner (p<0.05). The therapeutic time window of WEAA was 3 h in this ischemia-reperfusion rat model. WEAA also significantly inhibited increased neutrophil infiltration of ischemic brain tissue as estimated by myeloperoxidase (MPO) activity and immunohistochemical analysis. MPO-positive cells were markedly reduced by WEAA administration in striatal and cortical areas. These findings suggest that WEAA plays a crucial protective role in ischemia-induced brain injury, and suggest that WEAA could serve as a lead medicinal herb for the development of neuroprotective agents following transient focal ischemic brain injury.

Topics: Anemarrhena; Animals; Biphenyl Compounds; Brain; Disease Models, Animal; Dose-Response Relationship, Drug; Drugs, Chinese Herbal; Free Radical Scavengers; Hydrazines; Immunohistochemistry; Infarction, Middle Cerebral Artery; Ischemic Attack, Transient; Male; Neuroprotective Agents; Neutrophil Infiltration; Peroxidase; Picrates; Rats; Rats, Sprague-Dawley; Reperfusion Injury; Rhizome; Saponins; Time Factors; Triterpenes

A series of novel tetra substituted thiophenes were synthesized, characterized, and evaluated for their anti-inflammatory activity in carrageenin induced rat paw edema model-an acute in vivo model. Compounds V1, V3, V11, V12, V17, and V18 showed good anti-inflammatory activity, indicating the importance of oxime moiety in modulating the activity. The structure-activity relationship studies explore "the aliphatic oxime esters" attached via a ketone bridge to fifth position of the thiophene, and indicate that this feature may enhance the anti-inflammatory activity as compared to aromatic oximes. Since free radicals are implicated in various inflammatory disorders, the free radical scavenging activity of some of the synthesized candidates was assessed using 1,1-diphenyl-2-picryl hydrazyl assay. The oxime containing analogs exhibited weak to moderate activity as free radical scavengers in DPPH assay. A plausible reasoning for its free radical scavenging ability is discussed. All the compounds were also screened in nitro blue tetrazolium model, to assess them as superoxide anion radical scavengers. A direct correlation between anti-inflammatory activity and free radical scavenging activity was not seen. The results disclose a new class of anti-inflammatory agents designed and synthesized for the first time wherein the utility of aliphatic oxime esters in modulating the anti-inflammatory activity profile is apparent. This will give us potential anti-inflammatory leads.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Biphenyl Compounds; Disease Models, Animal; Drug Design; Edema; Esters; Free Radical Scavengers; Hydrocarbons, Aromatic; Molecular Structure; Oximes; Picrates; Rats; Structure-Activity Relationship; Thiophenes

The effects of purple sweet potato anthocyanin (SPA) and Cordyceps mushroom extract (CME) on lipid peroxidation, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals and cognitive deficits were examined. Both SPA and CME exhibited DPPH radical scavenging activities with similar potency. In contrast, only SPA was shown to effectively inhibit lipid peroxidation initiated by Fe2+ and ascorbic acid in rat brain homogenates. Furthermore, SPA markedly enhanced cognitive performance, assessed by passive avoidance test in ethanol-treated mice. Combined treatments with SPA and CME did not significantly influence the effects of SPA alone. These results demonstrate that anthocyanin prepared from purple sweet potato exhibits memory enhancing effects, which may be associated with its antioxidant properties.

Topics: Administration, Oral; Agaricales; Animals; Anthocyanins; Antioxidants; Avoidance Learning; Biphenyl Compounds; Brain; Cognition Disorders; Complex Mixtures; Cordyceps; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Therapy, Combination; Ethanol; Free Radical Scavengers; Hydroxyl Radical; Ipomoea batatas; Lipid Peroxidation; Male; Memory Disorders; Mice; Mice, Inbred ICR; Phytotherapy; Picrates; Plant Extracts; Rats; Rats, Sprague-Dawley

1. Dietary antioxidants are thought to be beneficial in reducing the incidence of coronary heart disease. In this study, we compared resveratrol and analogues on their antioxidation and free radical scavenging activities to their protective effects on ischaemia-reperfusion induced injuries of rat hearts. 2. Astringinin (3,3',4',5-tetrahydroxystilbene) was shown to be a more potent inhibitor than other analogues against Cu(2+)-induced LDL (low-density lipoprotein) oxidation, as measured by the formation of conjugated diene and TBARS (thiobarbituric acid-reactive substance) and by the electrophoretic mobility of the oxidized LDL. 3. Resveratrol (trans-3,4',5-trihydroxystilbene) and astringinin scavenged the stable free radical DPPH (1,1-diphenyl-2-picryl-hydrazyl) with an IC(0.200) of 7.1 and 4.3 microM, respectively. 4. Astringinin has a superoxide anion scavenging activity about 160 fold more potent than resveratrol. 5. After a 30 min global ischemia followed by 2 h reperfusion, astringinin (10 microM) significantly reduced infarct size, superoxide anion production and increased functional recovery of the coronary flow in Langendorff-perfused rat hearts. 6. The result showed there is a positive correlation between the anti-oxidation and cardioprotective activities among these phenolic compounds. Our finding together with the fact that astringinin is more water-soluble than resveratrol suggest that astringinin could potentially be used as an anti-oxidant and cardioprotective agent in biological systems.

Topics: Animals; Biphenyl Compounds; Disease Models, Animal; Free Radical Scavengers; Humans; Lipoproteins, LDL; Male; Myocardial Ischemia; Oxidation-Reduction; Picrates; Protective Agents; Rats; Rats, Inbred WKY; Reperfusion Injury; Resveratrol; Stilbenes; Superoxides

Salvia miltiorrhiza is a traditional Chinese medicine which has been well documented for its anti-cancer effects. Based on the structure of danshinone, one of the active compounds derived from Salvia miltiorrhiza, we synthesized a simplified phenolic analog, S-3-1, and tried to explore its possible actions in preventing the development of cancer. With the Ames test, S-3-1 was found to efficiently suppress the mutagenicity of benzo[alpha]pyrene. This result is consistent with the inhibitory effect of S-3-1 on the activation of benzo[alpha]pyrene by hepatic microsomal enzymes. Besides the anti-initiation effects, S-3-1 could significantly inhibit the croton oil-induced increase of mouse skin epithermal ornithine decarboxylase activity. Moreover, S-3-1 quenched both superoxide and hydroxyl free radicals whereas it inhibited lipid peroxidation in the in vitro model. These results suggest that S-3-1 might act as anti-initiation and anti-promotion agents through reversing the biochemical alterations induced by carcinogen during carcinogenesis. Therefore, we further investigated the effects of S-3-1 on carcinogenesis. In vitro, S-3-1 inhibited the benzo[alpha]pyrene-induced transformation of V79 Chinese hamster lung fibroblasts. At 10-40 mg/kg, S-3-1 was found to inhibit the development of DMBA/croton oil-induced skin papilloma in mice through decreasing the incidence of papilloma, prolonging the latent period of tumor occurrence and reducing tumor number per mouse in a dose-dependent manner. We concluded from this study that S-3-1 might be developed as a new chemopreventive drug.

Topics: 9,10-Dimethyl-1,2-benzanthracene; Animals; Anticarcinogenic Agents; Benzo(a)pyrene; Benzofurans; Bepridil; Biphenyl Compounds; Cell Transformation, Neoplastic; Cells, Cultured; Cricetinae; Croton Oil; Cysteine; Disease Models, Animal; Dose-Response Relationship, Drug; Drugs, Chinese Herbal; Epithelial Cells; Fibroblasts; Free Radical Scavengers; Hypoxanthine; In Vitro Techniques; Iron; Lipid Peroxidation; Lung; Male; Medicine, Chinese Traditional; Mice; Mice, Inbred ICR; Microsomes, Liver; Molecular Structure; Mutagens; Ornithine; Ornithine Decarboxylase; Papilloma; Pentetic Acid; Phenanthrenes; Picrates; Plants, Medicinal; Rats; Salmonella; Skin; Skin Neoplasms; Spectrometry, Mass, Electrospray Ionization; Structure-Activity Relationship; Xanthine Oxidase

1,1-Diphenyl-2-Picryl-Hydrazyl (DPPH), a stable free radical, has been used for detecting antioxidant activity in chemical analysis. However, it is still unknown if DPPH triggers free radical injury in cardiac tissue. In order to establish a simple free radical-injured isolated heart model, we investigated the action of DPPH on isolated guinea pig heart by Langendorff perfusion and compared it with cardiac effect of superoxide anion (O2.-), generated by the hypoxanthine (HX)-xanthine oxidase (XO) system. Free radical scavengers, dimethyl sulphoxide (DMSO), superoxide dismutase (SOD), and L-cysteine, were also used to analyze the characteristic of the DPPH free radical-derived cardiac dysfunction. In isolated guinea pig hearts, DPPH 100 nM and 250 nM in Krebs-Henseleit solution significantly decreased the left ventricular developed pressure (LVDP) and maximum velocity changes of left ventricular pressure (+/-LVdP/dtmax), elevated the left ventricular end-diastolic pressure (LVEDP), and increased lactate dehydrogenase (LDH) release and thiobarbituric acid-reactive substances (TBARS) formation in cardiac tissue. The cardiac dysfunction induced by DPPH 250 nM was more intense than 100 nM. L-Cysteine improved the DPPH-impaired cardiac function, while DMSO and SOD had no beneficial effect on this injury. The cardiac membrane fluidity was decreased by DPPH. Free radical signals, detected by electron spin resonance (ESR) in the DPPH-injured heart, were reduced by L-cysteine-treatment. These results suggest that DPPH free radical-induced cardiac dysfunction is attributed to neither the superoxide anion nor the hydroxyl radical. In conclusion, our data indicate that DPPH-induced isolated heart dysfunction serves as a simple and reproducible free radical-injured heart model.

Topics: Animals; Bepridil; Biphenyl Compounds; Cell Membrane Permeability; Coronary Circulation; Diastole; Disease Models, Animal; Electron Spin Resonance Spectroscopy; Free Radicals; Guinea Pigs; Heart Injuries; Heart Rate; L-Lactate Dehydrogenase; Male; Membrane Fluidity; Picrates; Systole; Thiobarbituric Acid Reactive Substances

Six substituted aryloxy diamines, synthesized as potential new antiinflammatory agents, were tested in vivo and in vitro in order to evaluate their biological activities. These derivatives reduced significant carrageenin rat paw edema and showed antiproteolytic activity. The in vitro inhibition of soybean lipoxygenase ranged from 41-77%. The results are discussed from the view of structural modifications.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Bepridil; Biphenyl Compounds; Diamines; Disease Models, Animal; Edema; Female; In Vitro Techniques; Lipoxygenase Inhibitors; Male; Picrates; Rats; Rats, Inbred F344; Soybean Proteins; Structure-Activity Relationship