1-1-diphenyl-2-picrylhydrazyl and Edema

Lipoxygenases (LO) have been implicated in several inflammatory diseases such as asthma, immune disorders, and cancers. Lipoxygenases play an essential role in the biosynthesis of the leukotrienes. Leukotrienes have been implicated as mediators in the pathophysiology of inflammatory diseases, host defense reactions and they were found to play important role in the propagation of the diseases states, exacerbating the local events and ultimately leading to tissue damage. As a consequence of these broad biological implications, there is a great interest in synthesising new compounds with this activity. The synthesis of new amides of aryl acetic acid is described. The structures of the synthesized compounds were confirmed by spectral and elemental analysis. Since lipophilicity is a significant physicochemical property determining distribution, bioavailability, metabolic activity and elimination, their lipophilicity is experimentally determined from RPTLC method. Several parameters were theoretically calculated and were used for a QSAR study. The compounds are tested in vitro on: a) soybean lipoxygenase inhibition, b) interaction with 1,1-diphenyl-2-picryl-hydrazyl (DPPH) stable free radical, c) the HO* mediated oxidation of DMSO, d) inhibition of lipid peroxidation, e) scavenging of superoxide anion radicals f) interaction with glutathione and g) in vivo for the inhibition of carrageenin induced rat paw edema. The compounds present significant antioxidant activities, medium anti-inflammatory activity and potent inhibition of soybean lipoxygenase as a result of their physicochemical features.

Topics: Amides; Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Biphenyl Compounds; Carrageenan; Chemical Phenomena; Chemistry, Physical; Edema; Female; Free Radical Scavengers; Glutathione; Hydroxyl Radical; Indicators and Reagents; Lipid Peroxidation; Lipoxygenase Inhibitors; Male; Mice; Oxidants; Picrates; Rats; Rats, Inbred F344; Spectrophotometry, Ultraviolet; Superoxides

There are several potential side and adverse effects are found to be associated with the anti-inflammatory drugs in clinical practice. The long-term use of these clinical agents highly unsafe. It encouraged the development of novel heterocyclic compounds with potential anti-inflammatory activity and low to no toxicity. In present investigation, a total of 12 indole functionalized pyrazole and oxadiazole derivatives were designed, synthesized and evaluated for the in-vivo anti-inflammatory and analgesic potential. These compounds displayed comparable anti-inflammatory and analgesic potential to the reference drugs. Finally, molecular docking analysis was performed considering different anti-inflammatory targets to determine the mechanistic target of the designed molecules. Detailed analysis suggested that the molecules inhibit COX-2, preferably over other anti-inflammatory targets. The results suggested that two compounds (15c and 15f) were found promising candidates for the development of novel anti-inflammatory agents.

Topics: Analgesics; Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Biphenyl Compounds; Carrageenan; Cattle; Cyclooxygenase 2; Dose-Response Relationship, Drug; Edema; Female; Humans; Indoles; Male; Molecular Structure; Oxadiazoles; Picrates; Pyrazoles; Rats; Rats, Wistar; Structure-Activity Relationship

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Arachidonate 5-Lipoxygenase; Biphenyl Compounds; Chemical Fractionation; Cyclic Nucleotide Phosphodiesterases, Type 5; Ear; Edema; Fatty Acids; Free Radical Scavengers; Mice; Picrates; Plant Oils; Seeds; Taxaceae

Asphodelus microcarpus is an important medicinal plant belonging to family Liliaceae. This plant is used in traditional medicine to treat abscesses by local application of the powder; the roots are used against white spots, and specifically used for ear pain.. The aim of the present study was to assess the in vitro antioxidant effects and the in vivo anti-inflammatory activity of the different parts methanolic extracts of the Asphodelus microcarpus: aerial part (APME), leaf (LME), stem flowers (SFME) and root (RME).. The antioxidant potency of extracts was evaluated by DPPH (2, 2-diphenyl-l-picrylhydrazyl), ABTS, β-carotene bleaching assays, iron chelating, free hydroxyl radicals (HO. The estimation of polyphenols and flavonoids showed that the leave methanolic extract contains a high amount of polyphenols and flavonoids: 755.3 ± 0.036 mg Gallic acid equivalent and 42.2 ± 0.043 mg Rutin equivalent/g of dried material, respectively. Oral administration of the APME and RME extract produced significant (p < 0.05) anti-edematogenic effect with a dose of 500 mg/kg in the carrageenan induced paw edema after 6 h (58.04%, 58.75%, respectively). APME, LME; SFME and RME extracts at 100, 300 and 500 mg/kg, exhibited significant (p < 0.05) inhibition of xylene induced ear edema.. the present study confirms the use of A. microcarpus in traditional medicine as anti-inflammatory agent.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Benzothiazoles; beta Carotene; Biphenyl Compounds; Carrageenan; Edema; Female; Hydroxyl Radical; Iron; Liliaceae; Mice; Phytotherapy; Picrates; Plant Components, Aerial; Plant Extracts; Rats, Wistar; Sulfonic Acids; Xylenes

Lycium europaeum Linn. is widely used to treat the burning of the skin and well-known as a medicinal plant having various biological activities.. The purpose of the present study is to characterize the polysaccharide from L. europaeum L. leaves (LEP) and to explore its antioxidant, anti-inflammatory and hepato-nephroprotective properties.. The structural and functional characteristics of LEP were investigated using X-ray diffraction techniques (XRD), Scanning Electron Microscopy (SEM), and FT-IR Spectroscopy. The antioxidant activity was evaluated using 2,2-diphenyl-1-picrylhydrazyl and hydrogen peroxide scavenging assays. Hepato-renal effects were studied using CCl. The LEP showed an interesting water-holding capacity and effective foaming and emulsifying properties. XRD analysis suggested that LEP form a semi-crystalline polymer with an amorphous structure. FT-IR profile showed the presence of pyranose ring in LEP. SEM and helix-coil transition analyses indicated that LEP had a lamellar structure with angular edges and didn't present a triple helical conformation in solution. In vitro, LEP indicated significant concentration-dependent antioxidant activity. In vivo, LEP treatment significantly reduced the effects of CCl. Overall, the findings of this study support the traditional use of L. europaeum L. This plant may also be used as a good agent for protection against inflammatory diseases and hepato-renal injuries in patients with cancer.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Carbon Tetrachloride; Carrageenan; Chemical and Drug Induced Liver Injury; Cisplatin; Edema; Hydrogen Peroxide; Kidney; Kidney Diseases; Liver; Lycium; Mice; Picrates; Plant Leaves; Polysaccharides

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

Trichilia silvatica, popularly known as "catiguá-branco", is distributed in Brazil (Mato Grosso do Sul), and members of this genus are commonly used for the treatment of rheumatism (arthritis). The aim of this research was to investigate the anti-inflammatory, antioxidant and antiproliferative activities of the methanolic extract of the leaves (MEL-TS) and bark (MEB-TS) of T. silvatica. We also evaluated the concentration of phenolic compounds, flavonoids, flavonol, and condensed tannins by liquid chromatography - photodiode array (LC/PDA) analysis.. The MEL-TS and MEB-TS revealed the presence of caffeic acid in both extracts by LC/PDA. The samples were evaluated for antioxidant activity using free-radical scavenging and lipoperoxidation assays. The anti-inflammatory effects were studied in carrageenan-induced paw edema, pleurisy and zymosan-induced arthritis.. The MEL-TS and MEB-TS showed the total phenolic concentration (270.8 ± 17.10 mg gallic acid equivalents GAE/g extract and 278.8 ± 25.13 mg GAE/ g extract, respectively), and flavonoids in MEL-TS (209.30 ± 2.91 mg quercetin equivalents QE/ g extract). In the lipoperoxidation assay, exhibited moderate antioxidant activity with IC50 values ≤ 35.32 µg/mL. Both extracts inhibited oedema induced by carrageenan at 2 h and 4 h, inhibited leukocyte migration at 6 h post administration, and did not impact zymosan-induced arthritis. Finally, MEL-TS was particularly effective against prostate cell line (GI50 ≤ 0.22 µg/mL).. Overall, the results indicated that T. silvatica reduce migration leukocytes activity, edema formation in these models of experimental arthritis could explain the popular use for treatment of inflammatory processes (rheumatism).

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Brazil; Cell Line, Tumor; Cell Proliferation; Edema; Female; Free Radicals; Humans; Male; Meliaceae; Mice; Picrates; Plant Bark; Plant Extracts; Plant Leaves; Pleurisy

Topics: Analgesics; Animals; Anti-Inflammatory Agents; Antioxidants; Benzothiazoles; Biphenyl Compounds; Edema; Hydroxides; Inflammation; Male; Methanol; Mice; Ononis; Phytotherapy; Picrates; Plant Extracts; Plant Roots; Rats; Rats, Sprague-Dawley; Skin; Sulfonic Acids; Wound Healing

Inflammation activated by oxidative stress can cause various diseases, such as asthma, rheumatoid arthritis, cancer, diabetes, etc. Plant constituents with sesquiterpene lactones possess antioxidant and anti-inflammatory properties.. To determine the antioxidant and anti-inflammatory potential of isolated phytoconstituent from Cyathocline purpurea Buch-Ham ex D (CP). Don in laboratory animals. Furthermore, to understand the interactions involved in the binding of this compound to cyclooxygenase-2 (COX-2) via computational docking.. Phytoconstituent was isolated, purified and well characterized (using IR, NMR, and MS) from ethyl acetate fraction of CP methanolic extract. It was then evaluated for its in-vitro antioxidant activity against 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydrogen peroxide (H. The presence of hydroxyl group in HGN provides a credential to its in-vivo anti-inflammatory and in-vitro antioxidant activities. Furthermore, the good binding affinity of HGN for the active site of COX-2 may open novel vistas in therapeutic option with natural antioxidants like Cyathocline purpurea to treat various inflammatory disorders.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Asteraceae; Biphenyl Compounds; Carrageenan; Cells, Cultured; Cyclooxygenase 2; Edema; Female; Humans; Hydrogen Peroxide; Inflammation; Male; Mice; Oxidative Stress; Phytotherapy; Picrates; Rats; Rats, Wistar; Sesquiterpenes, Guaiane

Saponins are the main constituents of genus Sapindus and have the therapeutic potential for inflammatory disorders. In this study the antioxidant, anti-inflammatory, analgesic and antipyretic potential of the stem bark of soap nut (Sapindus mukorossi) methanol extract and its derived fractions has been investigated.. Powder of stem bark of the S. mukorossi was extracted with methanol (SMM) and fractionated in order of n-hexane (SMH), chloroform (SMC), ethyl acetate (SME), n-butanol (SMB) and the remaining as aqueous fraction (SMA). Quantitative estimation for the total phenolic and total flavonoid content was carried out in all the extract/fractions. Further, various in vitro antioxidant assays were also performed. Anti-inflammatory (Carrageenan induced paw edema), analgesic (hot plate latency test) and antipyretic (rectal temperature) were determined in Sprague-Dawley rat.. Quantitative estimation of total phenolic contents in extract/fractions varied between 252.3 ± 2.41 mg of GAE/g - 594.16 ± 4.3 mg of GAE/g while the total flavonoids estimated were from 11.02 ± 1.3 mg of RUE/g to 96.9 ± 3.2 mg of RUE/g. Standard antioxidant assays such as scavenging of DPPH, hydroxyl radical, nitric oxide, phosphomolybdenum assay, reducing power, inhibition of β-carotene bleaching, iron chelation activity and inhibition of heat induced protein denaturation indicated the antioxidant potential of the extract/fractions. Carrageenan induced paw edema of rat was effectively inhibited by SMA at 300 mg/kg administration to rat (84.19 ± 1.48%) after 3 h and analgesia (latency time) in hot plate test (55.78 ± 1.22%) after 120 min. SMA at 300 mg/kg distinctly decreased the rectal temperature in brewer's yeast (Saccharomyces cerevisiae) induced pyrexia in rat.. The resulted obtained in this study suggested the therapeutic importance of stem bark of S. mukorossi in inflammatory related disorders.

Topics: Analgesics; Animals; Anti-Inflammatory Agents; Antioxidants; Antipyretics; Behavior, Animal; Biphenyl Compounds; Body Temperature; Edema; Female; Flavonoids; Male; Picrates; Plant Bark; Plant Extracts; Rats; Rats, Sprague-Dawley; Sapindus

Echinacea (Asteraceae) is used because of its pharmacological properties. However, there are few studies that integrate phytochemical analyses with pharmacological effects.. Evaluate the chemical profile and biological activity of hydroalcoholic Echinacea extracts.. The difference in the chemical and pharmacological properties among extracts highlights the need to consider strategies and policies for standardization of commercial herbal extracts in order to guarantee the safety and identity of this type of products.

Topics: Alloxan; Animals; Anti-Inflammatory Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Benzothiazoles; Biomarkers; Biphenyl Compounds; Blood Glucose; Carrageenan; Cell Proliferation; Diabetes Mellitus, Experimental; Echinacea; Edema; HeLa Cells; Humans; Hypoglycemic Agents; Male; MCF-7 Cells; Neoplasms; Phytochemicals; Phytotherapy; Picrates; Plant Extracts; Plants, Medicinal; Rats, Wistar; Sulfonic Acids; Time Factors

Solanum corymbiflorum is popularly known as "baga-de-veado" and its leaves are applied on inflamed legs, scabies, tick bite, boils, mastitis, low back pain and otitis. The aim of this study was evaluate anti-inflammatory in vivo activity and relate this activity with antioxidant compounds present in the extract of S. corymbiflorum leaves. The extract from S. corymbiflorum leaves topically applied was able to reduce the croton oil-induced ear edema and myeloperoxidase (MPO) activity with maximum inhibition of 87±3% and 45±7%, rescpectively in the dose of 1mg/ear. Similar results were found for positive control dexamethasone, which presented inhibitions of ear edema and MPO activity of 89±3% and 50±3%, respectively in a dose of 0.1mg/ear. These findings are due, at least in part, the presence of polyphenols (195.28mg GAE/g) and flavonoids, as chlorogenic acid (59.27mg/g), rutin (12.72mg/g), rosmarinic acid, caffeic acid and gallic acid found by high performance liquid chromatography (HPLC) analysis. This species showed potencial antioxidant by 1,1-diphenyl-2-picrylhydrazyl (DPPH), and carbonyl groups in proteins methods which may be related with the presence of this compounds. This species possess anti-inflammatory activity confirming their popular use for the local treatment of skin inflammatory disorders.

Topics: Administration, Topical; Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Chromatography, High Pressure Liquid; Dexamethasone; Edema; Flavonoids; Male; Mice; Peroxidase; Picrates; Plant Extracts; Plant Leaves; Polyphenols; Protein Carbonylation; Solanum

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 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 development of new drugs to treat painful and inflammatory clinical conditions continues to be of great interest. The present study evaluated the antinociceptive and anti-inflammatory effects of 4-phenylselenyl-7-chloroquinoline (4-PSQ). Mice were orally (p.o.) pretreated with 4-PSQ (0.1-25mg/kg), meloxicam (25mg/kg, a reference drug) or vehicle, 30min prior to the acetic acid, formalin, hot-plate and open-field tests. 4-PSQ reduced abdominal writhing induced by acetic acid and it caused an increase in latency time in the hot-plate test. 4-PSQ inhibited early and late phases of nociception and reduced the paw edema caused by formalin. Locomotor and exploratory activities in the open field test were not altered by treatments. In addition, a time-response curve was carried out by administration of 4-PSQ (25mg/kg; p.o.) at different times before the acetic acid injection. The antinociceptive effect in inhibiting acetic acid-induced abdominal writhing of 4-PSQ started at 0.5h and remained significant up to 4h after administration. Indeed, the anti-inflammatory and antioxidant properties of 4-PSQ were investigated. 4-PSQ diminished the edema formation and decreased the myeloperoxidase activity and reactive species levels induced by croton oil in the ear tissue. 4-PSQ partially protected against the decrease of the 2,2'-Azinobis-3-ethylbenzothiazoline 6-sulfonic acid (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) levels induced by croton oil. Meloxicam presented similar results for 4-PSQ in tests evaluated. These results demonstrated that 4-PSQ exerts acute anti-inflammatory and antinociceptive actions, suggesting that it may represent an alternative in the development of future new therapeutic strategies.

Topics: Analgesics; Animals; Anti-Inflammatory Agents; Behavior, Animal; Benzothiazoles; Biphenyl Compounds; Edema; Male; Mice; Organoselenium Compounds; Peroxidase; Picrates; Quinolines; Sulfonic Acids

Moussonia deppeana, known as Tlachichinole, is a Mexican medicinal plant used for treatment of inflammatory diseases, influenza, diarrhea, gastrointestinal disorders and arthritis.. In this paper the antioxidant and anti-inflammatory activities as well as the acute and sub-acute toxicological effects were evaluated for the ethanolic extract from aerial parts of M. deppeana, also its phytochemical analysis is described.. Phytochemical analysis and compound isolation were performed with thin layer chromatography. The chemical identification of the main compound was performed by (1)H NMR (COSY, NOESY, HSQC and HMBC) spectra. In vitro antioxidant capacity and total phenolic content for the ethanolic extract and its primary fractions was determined by DPPH and Folin-Ciocalteu reagent. Acute and subacute toxicity tests were evaluated on Balb/C mice. Finally acute anti-inflammatory evaluation was tested for a local (TPA) and systemic (carrageenan) murine model.. The main compound isolated from the ethanolic extract of M. deppeana was Verbascoside, which was isolated from F3 and was identified by (1)H NMR and COSY data. Furthermore oleanolic and ursolic acids were isolated from primary fractions F1 and F2. Ethanolic extract showed IC50 = 6.71mg/mL for DPPH test and 664.12µg QE/mL for the total phenolic content. The LD50 value was >2g/kg by i.g. route in male and female mice. Sub-acute administration (28 days) of the ethanolic extract (1g/kg) did not cause lethality or alter any hematological and biochemical parameters, in addition, histological analysis of the major organs exhibited no structural changes. Anti-inflammatory activity of the ethanolic extract showed an ED50 = 1.5mg/ear and 450mg/kg for TPA and carrageenan test, respectively. Primary fractions generated moderate local and systemic anti-inflammatory activity.. The ethanolic extract from the aerial parts of M. deppeana did not cause any lethality or adverse effect in either of the acute and sub-acute toxicity tests. This exhibited an important local and systemic anti-inflammatory activity and also moderate antioxidant capacity. Moreover, the primary fraction F2 was more active for the TPA model while the primary fraction F3 was most active in the carrageenan model in vivo. The main compound isolated from F3 was verbascoside; on the other hand also ursolic and oleanolic acids were isolated from F1 and F2.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Carrageenan; Edema; Female; Glucosides; Magnoliopsida; Male; Medicine, Traditional; Mexico; Mice, Inbred BALB C; Oleanolic Acid; Phenols; Phorbol Esters; Phytochemicals; Phytotherapy; Picrates; Plant Components, Aerial; Plant Extracts; Triterpenes; Ursolic Acid

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

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

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

A series of bipyrazoles functionalized with sulfonamide, N(1),N(3)-disubstituted sulfonylurea, sulfonylthiourea pharmacophores, and some derived thiazolidinone and thiazoline ring systems were synthesized. The structures of the newly synthesized compounds were substantiated by analytical and diverse spectroscopic data. The anti-inflammatory and antioxidant activity of some of the newly synthesized compounds were tested and the results reveled that compounds 14, 16, 20, 24 and 25 proved to be the most active anti-inflammatory agents according to the Carrageenan-induced rat paw edema bioassay. Whereas, the analogs 14, 16 and 24 were able to exhibit good to moderate antioxidant activity in the DPPH radical-scavenging assay. Hence, compounds 14, 16 and 24 can be considered as lead structures for dual anti-inflammatory and antioxidant activities.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Biphenyl Compounds; Chalcones; Edema; Free Radicals; Male; Picrates; Pyrazoles; Rats

Cinnamic acids have been identified as interesting compounds with cytotoxic, anti-inflammatory, and antioxidant properties. Lipoxygenase pathway, catalyzing the first two steps of the transformation of arachidonic acid into leukotrienes is implicated in several processes such as cell differentiation, inflammation and carcinogenesis. Development of drugs that interfere with the formation or effects of these metabolites would be important for the treatment of various diseases like asthma, psoriasis, ulcerative colitis, rheumatoid arthritis, atherosclerosis, cancer, and blood vessel disorders. Till now, asthma consists of the only pathological case in which improvement has been shown by lipoxygenase LO inhibitors. Thus, the research has been directed towards the development of drugs that interfere with the formation of leukotrienes. In order to explore the anti-inflammatory and cytotoxic effects of antioxidant acrylic/cinnamic acids a series of derivatives bearing the appropriate moieties have been synthesized via the Knoevenagel condensation and evaluated for their biological activities. The compounds have shown important antioxidant activity, anti-inflammatory activity and very good inhibition of soybean lipoxygenase while some of them were tested for their anticancer activity.

Topics: Acetic Acid; Animals; Anti-Inflammatory Agents; Antineoplastic Agents; Antioxidants; Arachidonic Acid; Biphenyl Compounds; Cell Line, Tumor; Cinnamates; Cyclooxygenase 1; Edema; Free Radical Scavengers; Glycine max; Heme; Humans; Hydroxyl Radical; Lipid Peroxidation; Lipoxygenase; Lipoxygenase Inhibitors; Picrates; Rats

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

Within the framework of our attempts to synthesize pleiotropic anti-inflammatory agents, we have synthesized some chalcones and their corresponding 3,4-pyrrolyl derivatives. Chalcones constitute a class of compounds with high biological impact. They are known for a number of biological activities, including anti-inflammatory and free radical scavenging activities. They inhibit several enzymes implicated in the inflammatory process, such as lipoxygenase, cyclooxygenase (COX) and lysozymes. The synthesized pyrroles have been studied for: (1) their in vitro inhibition of lipoxygenase; (2) their in vitro inhibition of COX; (3) their in vitro inhibition of lipid peroxidation; (4) their interaction with the stable, N-centered, free radical, 2,2-diphenyl-1-picrylhydrazyl (DPPH); (5) their inhibition on interleukin-6 (IL-6); (6) their anti-proteolytic activity; and (7) their in vivo anti-inflammatory activity using carrageenan-induced rat paw edema. Their physicochemical properties were determined to explain the biological results. Lipophilicity was experimentally determined. 2i and 2v were found to be promising multifunctional molecules with high antiproteolytic and anti-inflammatory activities in combination with anti-interleukin-6 activity.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Carrageenan; Chalcones; Edema; Lipid Peroxidation; Lipoxygenase; Picrates; Prostaglandin-Endoperoxide Synthases; Pyrroles; Rats

Cnidoscolus chayamansa Mc Vaugh (Euphorbiaceae) is commonly known as 'chaya' in Central America. In South East Mexico, because of its high nutritional values, is an important part of the diet of many indigenous communities. Chaya is also used as a traditional remedy for the treatment of diabetes, rheumatism, gastrointestinal disorders and inflammation-related diseases. Although Cnidoscolus chayamansa is one of most used and valued medicinal plants, only few studies on documenting its pharmacological properties can be found.. Dried leaves of Cnidoscolus chayamansa were subjected to a successive maceration using Hex, EtOAc and EtOH. The antioxidant activities of the extracts were tested using the DPPH radical scavenging, Ferric reducing/antioxidant power and total phenolic content assays. To determine the anti-inflammatory activity, the TPA-induced mouse ear edema and the carrageenan-induced mouse paw edema assays were used. The cardioprotective effects of the EtOH extract was determined using the ischemia/reperfusion (I/R) rat model. Finally, the acute toxicity was determined using Lorke's method.. The results showed a similar anti-inflammatory activity (≈30%) for all extracts but only the EtOAc extract showed relevant activity when applied intraperitoneally. When tested for their antioxidant activity none of the extracts showed a significant activity suggesting that the antinflammatory activity is not related to a direct free radical scavenging of the extracts. Additionally, the EtOH extract showed a strong cardioprotective effect at 500mg/kg when given orally. Both the EtOAc and the EtOH extract have a LD50 >5g/kg, confirming their safety in acute oral administration.. All these results are relevant for a better understanding of the therapeutic used of Cnidoscolus chayamansa in the Mexican traditional medicine and highlights its cardioprotective potential.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Cardiotonic Agents; Carrageenan; Ear; Edema; Euphorbiaceae; Male; Medicine, Traditional; Mexico; Mice; Phenols; Phytotherapy; Picrates; Plant Extracts; Plant Leaves; Rats; Rats, Wistar; Reperfusion Injury; Tetradecanoylphorbol Acetate; Toxicity Tests, Acute

In the present study, the pharmacological effects of 2,8-dihydroxy-1,6-dimethoxyxanthone from the bark of Haploclathra paniculata were investigated in mice using in vivo inflammation and nociception models. Acetic acid-induced writhing, paw licking induced by formalin, hot plate, and carrageenan-induced paw edema tests were used to investigate the anti-inflammatory and antinociceptive activities of the xanthone compound. Xanthone, at both doses, inhibited abdominal writhing and the formalin test. At a dose of 20 mg/kg, the time of reaction to the hot plate increased, and significant effects were observed after 30, 60 and 90 min of treatment. At doses of 10 and 20 mg/kg p.o., the 2,8-dihydroxy-1,6-dimethoxyxanthone significantly reduced paw edema at 3 h after the stimulus. The tests also showed no acute toxicity of the xanthone compound in mice. 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging ability was also studied and confirmed the antioxidant activity of the xanthone. To propose the mechanism of action of anti-inflammatory activity of the xanthone, a molecular docking was performed using the isoenzymes cyclooxygenase 1 and 2 and the results indicate that the molecule is capable of inhibiting both the enzymes. Therefore, it can be concluded that 2,8-dihydroxy-1,6-dimethoxyxanthone from H. paniculata demonstrates analgesic, anti-inflammatory, and antioxidant activities.

Topics: Acetic Acid; Analgesics; Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Carrageenan; Clusiaceae; Cyclooxygenase 2 Inhibitors; Edema; Hot Temperature; Inflammation; Male; Pain; Pain Measurement; Phytotherapy; Picrates; Plant Bark; Plant Extracts; Prostaglandin-Endoperoxide Synthases; Rats, Wistar; Xanthones

The aim of the study was to investigate the anti-rheumatoid arthritic activity of four flavonoids from Daphne genkwa (FFD) in vivo and in vitro. Flavonoids of D. genkwa were extracted by refluxing with ethanol and purified by polyamide resin. An in vivo carrageenan-induced paw edema model, tampon-granuloma model and Freund's complete adjuvant (FCA)-induced arthritis mouse model were used to evaluate the anti-rheumatoid arthritic activities of FFD. Moreover, nitric oxide (NO) release and neutral red uptake (NRU) in lipopolysaccharide (LPS)-induced murine macrophage RAW264.7 cells were used to evaluate the anti-inflammatory effect in vitro. In addition, antioxidant effect of FFD was determined using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method. A high dose of FFD significantly reduced the degree of acute inflammatory paw edema in mice as a response to carrageenan administration (p<0.01). FFD displayed a dose-dependent inhibition of granuloma formation in mice (p<0.05). FFD also inhibited chronic inflammation in adjuvant-induced arthritis rats when administered orally at the dose of 50mg/kg/day (p<0.001). In addition, FFD suppressed the production of NO and exhibited immunoregulatory function in LPS-activated RAW264.7 cells in a dose-related manner. Simultaneously, FFD revealed conspicuous antioxidant activity with IC50 values of 18.20μg/ml. FFD possesses significant anti-inflammatory and antioxidant activity, which could be a potential therapeutic agent for chronic inflammatory disorders such as rheumatoid arthritis.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Antirheumatic Agents; Arthritis, Experimental; Arthritis, Rheumatoid; Biphenyl Compounds; Carrageenan; Daphne; Dose-Response Relationship, Drug; Edema; Female; Flavonoids; Freund's Adjuvant; Inflammation; Lipopolysaccharides; Macrophages; Male; Mice; Nitric Oxide; Phytotherapy; Picrates; Plant Extracts; Rats

Because atherosclerosis is an inflammatory process involving a series of pathological events such as dyslipidemia, oxidative stress, and blood clotting mechanisms, we hereby report the synthesis and evaluation of novel compounds in which antioxidant, anti-inflammatory, and squalene synthase (SQS) inhibitory/hypolipidemic activities are combined in simple molecules through design. The coupling of two different pharmacophores afforded compounds 1-12, whose biological profile was markedly improved compared to those of parent lead structures (i.e., the hypolipidemic 2-hydroxy-2-aryl-(benzo)oxa(or thia)zine and the antioxidant phenothiazine). Most derivatives strongly inhibited in vitro microsomal lipid and LDL peroxidation, exhibiting potent free-radical scavenging activity. They further significantly inhibited SQS activity and showed remarkable antidyslipidemic activity in vivo in animal models of acute and high-fat-induced hyperlipidemia. Finally, several compounds showed anti-inflammatory activity in vitro, inhibiting cycloxygenase (COX-1/2) activity. The multimodal properties of the new compounds and especially their combined antioxidant/SQS/COX inhibitory activity render them interesting lead compounds for further evaluation against atherosclerosis.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Atherosclerosis; Biphenyl Compounds; Carrageenan; Cholesterol, Dietary; Cyclooxygenase Inhibitors; Diet, High-Fat; Drug Design; Edema; Enzyme Inhibitors; Farnesyl-Diphosphate Farnesyltransferase; Hypolipidemic Agents; In Vitro Techniques; Indicators and Reagents; Lipid Peroxidation; Magnetic Resonance Spectroscopy; Male; Mice; Microsomes; Phenothiazines; Picrates; Rats

Based on the fact that Synadenium grantii is used in folk medicine for the treatment of peptic ulcers and inflammatory diseases, this work describes its chemical and pharmacological properties. Pharmacological investigation of the crude bark extract showed a high antioxidant activity over several scavenger systems, such as 2,2'-azino-bis (3-ethylenebenzothiazoline-6-sulfonic acid)• +, 1-diphenyl-2-picrylhydrazyl•, O2 • - , and HOCl, as well as an enzymatic system with human myeloperoxidase and an ex vivo hemolysis system. Furthermore, the oral administration of the crude bark extract was able to reduce carrageenan-induced rat paw edema as effectively as ibuprofen. These biological activities may be associated with the presence of flavonoids and terpenes, as revealed by HPLC and NMR analyses of the crude stem bark extract. The phytochemical investigations in this study resulted in the isolation of friedelin and 3β-friedelinol for the first time, while euphol and lanosterol were also isolated.

Topics: Administration, Oral; Animals; Anti-Inflammatory Agents; Antioxidants; Benzothiazoles; Biphenyl Compounds; Carrageenan; Edema; Euphorbia; Female; Flavonoids; Humans; Inflammation; Lanosterol; Peroxidase; Phytotherapy; Picrates; Plant Bark; Plant Extracts; Plant Stems; Rats, Wistar; Sulfonic Acids; Triterpenes

Inhibition of oxidative stress and inflammation in vascular endothelial cells (ECs) may represent a new therapeutic strategy against endothelial activation. Sinapic acid (SA), a phenylpropanoid compound, is found in natural herbs and high-bran cereals and has moderate antioxidant activity. We aimed to develop new SA agents with the properties of antioxidation and blocking EC activation for possible therapy of cardiovascular disease. We designed and synthesized 10 SA derivatives according to their chemical structures. Preliminary screening of the compounds involved scavenging hydroxyl radicals and 2,2-diphenyl-1-picrylhydrazyl (DPPH(⋅)), croton oil-induced ear edema in mice, and analysis of the mRNA expression of adhesion molecules in ECs. 1-Acetyl-sinapic acyl-4-(3'-chlorine-)benzylpiperazine (SA9) had the strongest antioxidant and anti-inflammatory activities both in vitro and in vivo. Thus, the effect of SA9 was further studied. SA9 inhibited tumor necrosis factor α-induced upregulation of adhesion molecules in ECs at both mRNA and protein levels, as well as the consequent monocyte adhesion to ECs. In vivo, result of face-to-face immunostaining showed that SA9 reduced lipopolysaccharide-induced expression of intercellular adhesion molecule-1 in mouse aortic intima. To study the molecular mechanism, results from luciferase assay, nuclear translocation of NF-κB, and Western blot indicated that the mechanism of the anti-inflammatory effects of SA9 might be suppression of intracellular generation of ROS and inhibition of NF-κB activation in ECs. SA9 is a prototype of a novel class of antioxidant with anti-inflammatory effects in ECs. It may represent a new therapeutic approach for preventing endothelial activation in cardiovascular disorders.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Aorta; Biphenyl Compounds; Cell Adhesion; Coumaric Acids; Croton Oil; Ear; Edema; Endothelial Cells; Endothelium, Vascular; Free Radical Scavengers; Human Umbilical Vein Endothelial Cells; Humans; Inflammation; Intercellular Adhesion Molecule-1; Lipopolysaccharides; Mice; Mice, Inbred BALB C; Mice, Inbred C57BL; Monocytes; NF-kappa B; Oxidative Stress; Picrates; Tumor Necrosis Factor-alpha

Herein, we report the antioxidant properties of some selected substituted 2-indolyl carbohydrazides (JL34, JL40, JL71, JL87, JL317, JL432, JL436), the substituted 3-indolyl carbohydrazide JL344, 3-(3-hydrazinylpropyl)-1H-indole (JL72) and 3-(1H-indol-3-yl)propanehydrazide (JL418), throughout the assessment of their antioxidative potential using different antioxidant assays such as DPPH, lipid peroxidation in the APPH, or the DMSO method. We conclude that these compounds are convenient templates for the design of useful drugs in to treat Alzheimer's disease (AD), a pathology characterized by extensive oxidative stress and inflammation, thus essentially affected by reactive oxygen species (ROS). Most of them are potent hydroxyl radical scavengers and inhibit in vitro lipid peroxidation. Compounds JL40 and JL432 presenting higher lipoxygenase inhibitory activity among the tested derivatives, were found to present a promising anti-inflammatory in vivo result, as well as antioxidant and LOX inhibitory profile. These results in combination to their known AChE/BuChE inhibitory activities led us to propose these indolyl carbohydrazides as new multifunctional compounds against AD.

Topics: Alzheimer Disease; Animals; Antioxidants; Biocatalysis; Biphenyl Compounds; Carrageenan; Edema; Female; Free Radical Scavengers; Humans; Hydrazines; Lipid Peroxidation; Lipoxygenase; Male; Molecular Structure; Oxidation-Reduction; Picrates; Rats; Rats, Inbred F344; Structure-Activity Relationship

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

The polyherbal eye drop (Itone™) is a mixture of aqueous distillates of nineteen traditionally used ingredients that sum up to impart potency to the formulation and make it a useful adjunct in various ocular pathologies. However, as there have been no controlled experimental studies accounting to the above claim, therefore, the present study was designed to evaluate the polyherbal formulation (PHF) for antiangiogenic, anti-inflammatory, anticataract, antioxidant and cytotoxicity in addition to the evaluation of intraocular penetration of PHF in rabbit eyes using LC-MS/MS.. Antiangiogenic activity of the PHF was evaluated using in ovo chick chorio-allantoic membrane (CAM) assay and in vivo cautery induced corneal neovascularization assay in rats. Anticataract potential was evaluated using steroid induced cataract in developing chick embryos, sodium selenite induced cataract in rat pups and galactose induced cataract in rats. The antioxidant activity was evaluated using di-phenyl picryl hydrazyl (DPPH) radical scavenging assay. Anti-inflammatory activity was evaluated in vitro using inhibition of LTB4 formation in human WBCs and in vivo using carrageenan induced paw edema assay in rats. The cytotoxicity was evaluated against HeLa cancer cell lines using (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Furthermore evaluation of the intraocular penetration of the PHF was carried out in rabbit eyes via aqueous humor paracentesis and further analysis using LC-MS/MS.. PHF significantly inhibited VEGF induced proliferation of new blood vessels in CAM assay and inhibited the cautery induced corneal neovascularization in rats. Additionally, PHF showed noticeable delay in the progression of cataract in the selenite and galactose induced cataract models whereby the PHF treated lenses were graded for stages II and III respectively. However, the PHF did not show any anticataract activity in the hydrocortisone induced cataract model. Moreover, PHF exhibited anti-inflammatory activity whereby it showed 39.34% inhibition of LTB4 formation and significantly inhibited carrageenan induced paw edema in rats. Eight compounds of PHF viz. camphor, casticin, curcumin-II, quercetin, rosmarinic acid, γ-terpinene, β-pinene and dipentene exhibited transcorneal penetration in rabbit eyes.. The significant antiangiogenic and anti-inflammatory activities evinced by the PHF merits further investigation for ocular neovascular and inflammatory diseases in humans.

Topics: Angiogenesis Inhibitors; Animals; Anti-Inflammatory Agents; Aqueous Humor; Biphenyl Compounds; Blood Vessels; Carrageenan; Cataract; Chick Embryo; Cornea; Edema; Eye; Female; Galactose; HeLa Cells; Humans; Hydrocortisone; Inflammation; Lens, Crystalline; Leukocytes; Leukotriene B4; Male; Medicine, Ayurvedic; Models, Animal; Ophthalmic Solutions; Phytotherapy; Picrates; Plant Extracts; Rabbits; Rats; Rats, Wistar; Sodium Selenite; Steroids; Vascular Endothelial Growth Factor A

Annona dioica St. Hill (Annonacaeae) is a Brazilian plant used in folk medicine for the treatment of several types of rheumatisms and diarrhoea. The focus of this work was to evaluate the in vitro antiproliferative and antioxidant activity and the in vivo hypoglycaemic and anti-inflammatory activity of A. dioica and identify the principal constituents of this plant.. The crude methanol extract (EAD) and hexane (HF), chloroform (CF), ethyl acetate (EAF) and hydromethanol fractions (HMF) were evaluated for free radical scavenging activity using the DPPH assay. The EAD and EAF were assayed for hypoglycaemic activity in rats. The EAD was tested in an antiproliferation assay and for anti-inflammatory effects in paw oedema, in addition to myeloperoxidase activity induced by carrageenan (Cg) in mice. The EAF was assayed using chromatographic methods.. The fractionation of the EAF through chromatographic methods identified derivatives of the flavonoids quercetin and kaempferol. Among all the tested fractions, the ethyl acetate and hydromethanol fractions were the most potent, exhibiting an IC50 of 8.53 and 10.57 μg/mL, respectively, which is comparable to that of the commercial antioxidant butylated hydroxytoluene (BHT). The oral administration of the EAD (100 mg/kg) and EAF (15 mg/kg) inhibited the increase of glucose levels, resulting in a hypoglycaemic effect. The EAD (30 to 300 mg/kg) exhibited an anti-oedematogenic effect in Cg-induced paw oedema in a time- and dose-dependent manner. The results showed a reduction of MPO activity by A. dioica 6 h after the induction of paw oedema at all doses tested with maximal inhibition at 300 mg/kg.. Our results reveal for the first time that compounds contained in the A. dioica leaves exert anti-inflammatory, hypoglycaemic, antiproliferative, and antioxidant effects. The antioxidant activity may be associated with the presence of flavonoids.

Topics: Animals; Annona; Anti-Inflammatory Agents; Antineoplastic Agents, Phytogenic; Biphenyl Compounds; Blood Glucose; Carrageenan; Cell Line, Tumor; Dose-Response Relationship, Drug; Edema; Free Radical Scavengers; Hypoglycemic Agents; Inhibitory Concentration 50; Kaempferols; Male; Mice; Neoplasms; Peroxidase; Phytotherapy; Picrates; Plant Extracts; Quercetin; Rats; Rats, Wistar

Various parts of the perennial herb Hilleria latifolia (Lam.) H. Walt. (Family: Phytolaccaceae) are used in Ghanaian traditional medicine for the treatment of several inflammatory-related disorders. The present study examined the anti-inflammatory effect of an ethanolic extract of the aerial parts of Hilleria latifolia (HLE) in acute and chronic inflammation models. Since free radicals and reactive oxygen species are implicated in inflammatory diseases, the antioxidant potential of HLE was also investigated in in vitro experimental models. HLE (10-300 mg kg(-1), p.o.), either preemptively or curatively, significantly inhibited carrageenan-induced foot oedema in 7-day old chicks. Similarly, the NSAID diclofenac (10-100 mg kg(-1), i.p.) and the steroidal anti-inflammatory agent dexamethasone (0.3-3 mg kg(-1), i.p.) dose-dependently reduced the oedema in both pre-emptive and curative treatments. In the Freund's adjuvant induced-arthritis model in rats, HLE as well as the positive controls, dexamethasone and methotrexate, showed significant anti-arthritic properties when applied to established adjuvant arthritis. HLE (10-300 mg kg(-1), p.o.) significantly reduced oedema in the ipsilateral paw of rats but failed to prevent systemic arthritic spread. The DMARD methotrexate (0.1-1 mg kg(-1), i.p.) and dexamethasone (0.3-3 mg kg(-1), i.p.) reduced significantly the total polyarthritic oedema as well as the spread of the arthritis from the ipsilateral to the contralateral paws of the treated animals. The extract (0.03-1.00 mg ml(-1)) exhibited Fe(3+) reducing activity, scavenged DPPH and prevented lipid peroxidation. These findings suggest that the extract exerts in vivo anti-inflammatory activity after oral administration and also has antioxidant properties which may contribute to its activity.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Arthritis, Experimental; Biphenyl Compounds; Carrageenan; Chickens; Chronic Disease; Dexamethasone; Dose-Response Relationship, Drug; Edema; Free Radicals; Ghana; Inflammation; Iron Compounds; Lipid Peroxidation; Male; Methotrexate; Phytolaccaceae; Phytotherapy; Picrates; Plant Components, Aerial; Plant Extracts

The methanol crude extract of the leaves of Ficus radicans Roxb. 'Variegata' (Moraceae) and the n-hexane, ethyl acetate and aqueous methanol fractions resulting from its fractionation were evaluated for their anti-inflammatory, molluscicidal and free-radical scavenging activities. The crude extract and fractions exhibited significant inhibition of inflammation in both croton oil (CO)-induced ear oedema in mice (p<0.001) and carrageenan-induced rat paw oedema models (p<0.01). The molluscicidal assay against Biomphalaria glabrata showed a weak activity for the n-hexane fraction (DL(50)= 400 µg mL(-1)). A moderated 1,1-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging activity was observed for the ethyl acetate fraction (IC(50)= 66.2 µg mL(-1)). Fractionation of the extracts through chromatographic methods afforded the coumarins 7-methoxycoumarin, 7-hydroxy-6-methoxycoumarin and methoxy-3,4-dihydrocoumarin, the steroids β-sitosterol and β-sitosterol 3-O-β-glucopyranoside, as well as a cinnamic acid derivative and a flavonoid identified as trans-4-methoxy-2-β-D-glucopyranosyloxy cinnamic acid and quercetin 3-O-β-D-xylopyranosyl-(1 → 2)-α-L-rhamnopyranoside, respectively. The compounds were identified on the basis of their NMR spectral data and comparison with those previously reported in the literature.

Topics: Animals; Anti-Inflammatory Agents; Biomphalaria; Biphenyl Compounds; Carrageenan; Cinnamates; Croton Oil; Drug Evaluation, Preclinical; Edema; Ficus; Free Radical Scavengers; Glucosides; Male; Mice; Molecular Structure; Molluscacides; Monosaccharides; Picrates; Plant Extracts; Plant Leaves; Quercetin; Rats; Rats, Wistar; Scopoletin; Sitosterols

The plant Krameria pauciflora MOC et. Sessé ex DC. is used as an anti-inflammatory and antidiabetic in traditional medicine. The aim of this study was to evaluate the in vivo anti-inflammatory and antidiabetic effects of a methanol extract from the roots of K. pauciflora. Dichloromethane and ethyl acetate extracts obtained by partitioning the methanol extract were also evaluated. Complete methanol and dichloromethane extracts showed anti-inflammatory effects at 3 mg/kg. An anti-inflammatory effect similar to indomethacin (10 mg/kg) was observed when the methanol and dichloromethane extracts, which contain a cycloartane-type triterpene and an sterol, were administered orally at several doses (3, 10, 30 and 100 mg/kg), whereas no anti-inflammatory effect was observed at any dose for the ethyl acetate extract, which contains catechin-type flavonoids. The antidiabetic effect of each extract was also determined. An antihyperglycaemic effect was observed in diabetic rats, but no effect in normoglycaemic animals was observed when the methanol extract was administrated at 30 mg/kg. All of the extracts exhibited radical scavenger activity. Additionally, constituents from all of the extracts were identified by NMR. This article supports the use of K. pauciflora as an anti-inflammatory because it exhibits a similar effect to indomethacin. However, its antidiabetic effect is not completely clear, although it could be useful for preventing diabetic complications.

Topics: Animals; Anti-Inflammatory Agents; Area Under Curve; Benzothiazoles; Biphenyl Compounds; Blood Glucose; Carrageenan; Diabetes Mellitus, Experimental; Edema; Foot; Free Radical Scavengers; Free Radicals; Hypoglycemic Agents; Krameriaceae; Male; Methanol; Picrates; Plant Extracts; Plant Roots; Rats; Rats, Wistar; Sulfonic Acids

Ammannia baccifera L. has been reported as folklore remedy for the treatment of inflammation and tumor in the state of Rajasthan, India.. The present study was designed to investigate the antioxidant, anti-inflammatory and anti-nociceptive effects of the methanol extract from the aerial parts of Ammannia baccifera under in vitro and in vivo models.. The in vitro antioxidant activity of the extract was measured using DPPH, superoxide, hydroxyl and nitric oxide radicals. The anti-inflammatory activity was evaluated using carrageenan induced paw edema. Analgesic activity of the methanol extract was estimated against acetic acid-induced writhing and hot plate methods.. The IC(50) value for free radical scavenging activity of this extract was significantly superior over the positive standards butylated hydroxyl anisole (BHA) and rutin. The extract exhibited significant anti-inflammatory and analgesic activities at the dose of 100 and 200mg/kg p.o. The analgesic effect of the higher dose of the extract (200mg/kg) was comparable with the standard drugs aspirin and morphine.. The present study scientifically validated the traditional use of this plant against inflammation.

Topics: Acetic Acid; Analgesics; Animals; Anti-Inflammatory Agents; Antioxidants; Behavior, Animal; Biphenyl Compounds; Carrageenan; Edema; Hot Temperature; India; Inflammation; Inhibitory Concentration 50; Lythraceae; Male; Medicine, Traditional; Mice; Mice, Inbred Strains; Pain; Phytotherapy; Picrates; Plant Extracts; Plants, Medicinal; Rats; Rats, Wistar; Reactive Oxygen Species

A novel series of 3-(substituted)-aryl-5-(9-methyl-3-carbazole)-1H-2-pyrazolines (5a-o) has been synthesized and the structures of newly synthesized compounds were characterized by IR, (1)H NMR and mass spectral analysis. All the synthesized compounds were evaluated for their in vitro and in vivo anti-inflammatory activity, and also for their antioxidant activity. Compounds 5b, 5c, 5d and 5n were found to be selective COX-2 inhibitors. Compound 5c was found to potent inhibitor of the carrageenin induced paw edema in rats. Most of the compounds exhibited good DPPH and superoxide radical scavenging activity, while compounds 5c, 5d, 5i and 5k exhibited good hydroxyl radical scavenging activity. Molecular docking result, along with the biological assay data, suggested that compound 5c was a potential anti-inflammatory agent.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Biphenyl Compounds; Cyclooxygenase 1; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Dose-Response Relationship, Drug; Edema; Free Radical Scavengers; Models, Molecular; Molecular Structure; Picrates; Pyrazoles; Rats; Stereoisomerism; Structure-Activity Relationship; Superoxides

This study was designed to evaluate the anti-inflammatory action of four dihydroxy flavone derivatives; 3,3'- dihydroxy flavone, 5,6-dihydroxy flavone, 3,7-dihydroxy flavone and 6,3'-dihydroxy flavone and to further investigate the multiple cellular mechanisms underlying the anti-inflammatory effect of these compounds. The effect of dihydroxy flavones on acute inflammation was studied in rats employing carrageenan induced hind paw edema method. Further, the role of proinflammatory cytokines like TNF-α and IL-1β, cyclooxygenases (COX-1 and COX-2), and free radicals in the action of flavone derivatives was investigated using in vitro assays. All the four dihydroxy flavone derivatives exhibited time and dose dependent inhibition of carrageenan induced paw edema. In addition, the investigated compounds inhibited both the isoforms of cyclooxygenase and cytokines in a concentration dependent manner and also suppressed the release of reactive oxygen species. The anti-inflammatory effect of dihydroxy flavones may be through mechanisms that involve an interaction with cyclooxygenases, cytokines and reactive oxygen species.

Topics: Animals; Anti-Inflammatory Agents; Biphenyl Compounds; Cyclooxygenase 1; Cyclooxygenase 2; Cytokines; Dose-Response Relationship, Drug; Edema; Flavones; Free Radical Scavengers; Free Radicals; Hindlimb; Inflammation; Male; Nitrates; Picrates; Rats; Rats, Wistar

Pseudevernia furfuracea (L.) Zopf (Parmeliaceae) is a common epiphytic lichen in the conifer-hardwood forest of Anatolia. This species is used in traditional medicine in Turkey as a treatment for wounds, eczema and hemorrhoids.. The present study was designed to investigate the active compounds from Pseudevernia. furfuracea, and the isolation studies yielded atraric acid (Aslan et al., 2006) as the major compound and a mixture of methyl hematommate (Baumann, 1960) and methyl chlorohematommate (Bayır et al., 2006). Furthermore, methanolic extract from thalli of Pseudevernia. furfuracea and its fractions and isolates (Aslan et al., 2006; Baumann, 1960; Bayır et al., 2006) were investigated for in vitro antimicrobial and antioxidant activities, and in vivo antinociceptive, anti-inflammatory and wound healing activities.. Antimicrobial activities of the samples were determined by using the disc diffusion technique. 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay was used as a rapid TLC screening method to evaluate the antioxidant activity of Pseudevernia. furfuracea. The thiobarbituric acid (TBA) test was used to assess the efficacy of the extracts in protecting liposomes from lipid peroxidation. In vivo inhibitory effect of the extracts on the carrageenan-induced hind paw edema model in mice was studied for the assessment of anti-inflammatory activity. p-Benzoquinone-induced abdominal constriction test was used to explore the antinociceptive effects of the extracts. Moreover, the wound healing potential of the plant extracts that were evaluated by using in vivo incision and excision wound models on rats and mice, were comparatively assessed with a reference ointment Madecassol(®).. Significant antimicrobial activities were observed against Gram (+) microorganisms and Candida krusei and Candida. dubliniensis in dichloromethane (DCM) and ethyl acetate (EtOAc) extracts and isolates. The methanol (MeOH), DCM and EtOAc extracts of the lichen were found to possess moderate inhibitory activity on lipid peroxidation. Methanolic extract of the lichen was found to possess significant inhibitory activity on the carrageenan-induced hind paw edema model in mice whereas the other fractions did not show any activity. While DCM and EtOAc extracts and fractions showed notable anti-inflammatory activity on carrageenan-induced hind paw edema model without inducing any apparent acute toxicity or gastric damage. Moreover, topical application of the ointment prepared with MeOH extract and EtOAc fraction onto the incised wounds exerted remarkable wound healing activity.. The results of these experimental studies exhibited that nonpolar fractions of Pseudevernia. furfuracea have significant antimicrobial activity against especially Candida species and polar fractions (especially MeOH) display antioxidant, anti-inflammatory, antinociceptive and wound healing activities.

Topics: Analgesics; Animals; Anti-Infective Agents; Anti-Inflammatory Agents; Antioxidants; Ascomycota; Bacteria; Behavior, Animal; Benzoquinones; Biphenyl Compounds; Candida; Carrageenan; Complex Mixtures; Edema; Lichens; Male; Mice; Microbial Sensitivity Tests; Pain; Picrates; Rats; Rats, Sprague-Dawley; Skin; Thiobarbituric Acid Reactive Substances; Wound Healing

The standardized EtOAc, MeOH and 70% EtOH extracts of Tridax procumbens aerial parts showed significant inhibition of rat paw edema at a medium dose of 200mg/kg and the EtOAC extract was the most active. These extracts were standardized by HPLC with the help of chemical markers. Further, the extracts were evaluated for COX-1 and COX-2 inhibitory activity and EtOAc extract exhibited the highest inhibition of COX-1 and COX-2 at 50 μg/mL. Cent aurein, centaureidin and bergenin were isolated as COX-1 and COX-2 inhibitory principles from the EtOAc extract. The extracts also exhibited antioxidant activity against DPPH and ABTS free radicals. The anti-inflammatory activity of T. procumbens aerial parts could be at least in part due to COX-1, COX-2 enzyme inhibition and free radical-scavenging activities which may be attributed to the presence of flavonoids and other polyphenols in the extracts.

Topics: Animals; Antioxidants; Asteraceae; Benzothiazoles; Biphenyl Compounds; Chromatography, High Pressure Liquid; Cyclooxygenase Inhibitors; Edema; Female; Flavonoids; Phenols; Phytotherapy; Picrates; Plant Components, Aerial; Plant Extracts; Polyphenols; Rats; Rats, Sprague-Dawley; Sulfonic Acids; Thiazoles

Minocycline (Mino) and doxycycline (Dox) are second generation tetracyclines known to present several other effects, which are independent from their antimicrobial activities. We studied in a comparative way the anti-inflammatory effects of Mino and Dox, on acute models of peripheral inflammation in rodents (formalin test and peritonitis in mice, and carrageenan-induced paw oedema in rats). Immunohistochemical assays for TNF-alpha and iNOS in rat paws of carrageenan-induced oedema were also carried out as well as in vitro assays for myeloperoxidase (MPO) and lactate dehydrogenase (LDH). Furthermore, antioxidant activities were evaluated by the DPPH assay.. In the formalin test although Mino and Dox (1, 5, 10 and 25 mg/kg, i.p.) inhibited the first phase, they acted predominantly on the second phase of the test, where inhibition of the licking time close to 80% were observed. Mino and Dox were very efficacious in reducing the carrageenan-induced paw oedema in rats (10, 25 and 50 mg/kg, i.p.) and carrageenan-induced leucocyte migration (1 and 5 mg/kg, i.p.) to mice peritoneal cavities. Besides, they also significantly inhibited MPO and LDH releases at doses ranging from 0.001 to 1 μg/ml. Thus, in general, the anti-inflammatory activity of Dox was higher as compared to that of Mino, although the radical scavenging activity of Mino was of a magnitude 10 times higher.. Our data indicate that anti-inflammatory and antioxidant effects, involve the inhibition of iNOS and TNF-alpha, among other properties, and these encourage clinical studies of these compounds for new therapeutic applications, especially those were inflammation plays a role.

Topics: alpha-Tocopherol; Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Biphenyl Compounds; Carrageenan; Cell Movement; Doxycycline; Edema; Formaldehyde; Inflammation; L-Lactate Dehydrogenase; Male; Mice; Mice, Inbred Strains; Minocycline; Neutrophils; Nitric Oxide Synthase Type II; Oxidation-Reduction; Pain; Pain Measurement; Peritonitis; Peroxidase; Picrates; Rats; Rats, Wistar; Tumor Necrosis Factor-alpha

Areca catechu, commonly known as betel nut, is very famous for its medicinal use in multiple disorders. It is also popular as a remedy against inflammatory disorders in the Unani (Greco-Arab) system of medicine.. This study was aimed at investigating the anti-inflammatory and analgesic activities of the crude extract of Areca catechu and its respective fractions.. Paw edema, formalin-induced nociception and acetic acid-induced writhing assays were carried out in vivo. Free radical scavenging activity of the plant extract was performed in vitro.. Preliminary experiments using a single dose (100 mg/kg) of Areca catechu and its respective fractions demonstrated an anti-inflammatory effect on carrageenan-induced edema in mice and rats, the aqueous fraction being distinctly more effective. When studied on prostaglandin E₂ (PGE₂), arachidonic acid, histamine, or serotonin (5HT)-induced edema in rats, Areca catechu and its aqueous fraction markedly repressed only the PGE₂ and arachidonic acid-induced inflammation. When studied for analgesic activity, the crude extract and its aqueous fraction produced a dose-dependent (10-100 mg/kg) inhibitory effect on formalin-induced nociception in mice and acetic acid-induced writhing in rats, similar to aspirin. In DPPH assay, Areca catechu and its aqueous fraction exhibited free radical scavenging activity with respective IC(50) values of 5.34 μg/ml (4.93-5.78, CI; 95%, n=5) and 7.28 μg/ml (6.04-7.95, n=4), like that of rutin with IC(50) value of 4.75 μg/ml (3.89-5.42, n=4).. These results indicate the anti-inflammatory and analgesic effects of Areca catechu and provide a rationale for its medicinal use in inflammatory disorders.

Topics: Analgesics; Animals; Anti-Inflammatory Agents; Antioxidants; Areca; Aspirin; Behavior, Animal; Biphenyl Compounds; Carrageenan; Dose-Response Relationship, Drug; Edema; Mice; Mice, Inbred BALB C; Nuts; Pain; Phytotherapy; Picrates; Plant Extracts; Rats; Rats, Sprague-Dawley; Rutin

Aristotelia chilensis leaves (Elaeocarpaceae) are used in Chilean folk medicine to treat pain and inflammation. A bioguided study was carried out on serial extracts (hexane, dichloromethane, methanol, aqueous extract (INFU) and a crude mixture of alkaloids (ALK-MIX). All extracts were evaluated for (1) topical administration against both arachidonic acid and 12-deoxyphorbol-13-decanoate (TPA)-induced inflammation in mice and (2) per-os administration against inflammation by λ-carrageenan-induced paw oedema in guinea-pigs and (3) topical analgesia in tail flick and formalin models and per-os writhing test in mice.. Greater anti-inflammatory effects were obtained against TPA with dichloromethane extract and methanol extract (63.9 and 66.0%, respectively). INFU showed the most potent effect (56.2%) against arachidonic acid. Greater effects were obtained in the writhing test with hexane and dichloromethane extracts (89.2% both). In the topical analgesia models, all the extracts and ALK-MIX were active with exception of the hexane extract in the formalin assay. In tail flick test, ALK-MIX and the methanol extract were the most active (58.2 and 55.2%, respectively). In relation to the tail formalin assay, the methanol extract (74.1%) was the most active. Concerning antioxidant activity, both INFU and the methanol extract were the most active either in the inhibition of xanthine oxidase (52.9 and 62.7%, respectively) or in the DPPH free radical scavenging activity (EC50 (concentration that produced 50% of activity) = 12.1 and 9.7 µg/ml, respectively).. Aristoteline, aristone, serratoline and hobartinol were isolated from ALK-MIX. Ursolic acid, friedelin and quercetin 5,3'-dimethyl ether were present in the dichloromethane extract while quercetin 3-O-β-D-glucoside and kaempferol were present in the methanol extract. From INFU were isolated protopine, aristoteline and caffeic and ferulic acids.. The effects of A. chilensis are herein demonstrated, validating its use in traditional medicine. Protopine is reported for the first time in Elaeocarpaceae.

Topics: Administration, Topical; Alkaloids; Analgesia; Analgesics; Animals; Anti-Inflammatory Agents; Antioxidants; Arachidonic Acid; Behavior, Animal; Biphenyl Compounds; Carrageenan; Chile; Edema; Elaeocarpaceae; Female; Formaldehyde; Guinea Pigs; Inflammation; Male; Medicine, Traditional; Mice; Mice, Inbred Strains; Pain; Phorbol Esters; Phytotherapy; Picrates; Plant Extracts; Plant Leaves; Xanthine Oxidase

Malva parviflora L. (Malvaceae) is widely distributed throughout Africa. It has several uses in traditional medicinal practice. Leaves of this plant are used in the treatment of some inflammatory disorders.. The anti-inflammatory and the antioxidant activities of the methanol extract (Met. E) and aqueous extract (Aq. E) of M. parviflora leaves were investigated.. Croton oil-induced ear edema and acetic acid-induced vascular permeability were applied as acute inflammatory models to evaluate the anti-inflammatory activity of the extracts. The antioxidant effects were evaluated using the 1,1-diphenyl-2-picryl-hydrazyl (DPPH) radical assay and the measurement of the metal-chelating activity.. Results demonstrated that Met. E inhibited the croton oil-induced ear edema by 57%. In contrast, the Aq. E did not show any activity. Furthermore, Met. E and Aq. E inhibited significantly the acetic acid-induced vascular permeability by 36 and 40%, respectively. However, Met. E and Aq. E exerted a strong scavenging activity with IC(50) values of 89.03 ± 2.65 and 76.67 ± 0.29 µg/mL, respectively. Moreover, Met. E and Aq. E were able to chelate ferrous ions in a concentration-dependent manner.. These findings demonstrate that M. parviflora leaf extracts possess anti-inflammatory and antioxidant activities and thus have great potential as an interesting source for natural health products.

Topics: Africa; Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Capillary Permeability; Croton Oil; Dermatologic Agents; Ear; Edema; Free Radical Scavengers; Iron Chelating Agents; Malva; Mice; Phytotherapy; Picrates; Plant Extracts; Plant Leaves

[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

Nine compounds have been isolated from the ethyl acetate soluble fraction of C. sinensis, namely protocatechuic acid (1), trans-caffeic acid (2), methyl rosmarinate (3), rosmarinic acid (4), kaempferide-3-O-β-D-glucopyranoside (5), kaempferol-3-O-β-D-glucopyranoside (6), quercetin-3-O-β-D-glucopyranoside (7), kaempferide-3-O-α-L-rhamnopyranosyl (1→6)-β-D-glucopyranoside (8) and kaempferol-3-O-α-L-rhamno-pyranosyl (1→6)-β-D-glucopyranoside (9), all reported for the first time from this species. The structures of these compounds were deduced on the basis of spectroscopic studies, including 1D and 2D NMR techniques. Compounds 1-9 were investigated for biological activity and showed significant anti-inflammatory activity in the carrageen induced rat paw edema test. The antioxidant activities of isolated compounds 1-9 were evaluated by the DPPH radical scavenging test, and compounds 1, 2, 4 and 7-9 exhibited marked scavenging activity compared to the standard BHA. These compounds were further studied for their anti-glycation properties and some compounds showed significant anti-glycation inhibitory activity. The purity of compounds 2-5, 8 and 9 was confirmed by HPLC. The implications of these results for the chemotaxonomic studies of the genus Cordia have also been discussed.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Chromatography, High Pressure Liquid; Cordia; Edema; Glycosylation; Inhibitory Concentration 50; Phenols; Picrates; Rats

Water-soluble crude polysaccharide from a brown alga Turbinaria ornata (TCP) was screened for its antioxidant and anti-inflammatory potential. The major functional groups of polysaccharide were analyzed by Fourier Transmission-Infra Red (FT-IR). In vitro free radical quenching and total antioxidant activity of TCP was investigated by 1, 1-diphenyl-2-picryl hydrazyl (DPPH), nitric oxide (NO) scavenging, lipid peroxidation (LPO) inhibition and ABTS radical assay. Evaluation of anti-inflammatory activity of TCP was performed using carrageenan-induced paw edema in rats and vascular permeability test in mice. Phytochemical analysis of TCP showed the presence of carbohydrates, proteins and polyphenols further, the FT-IR analysis of TCP showed the presence of functional groups of sugar moiety, uronic acids and sulfate groups. TCP showed maximum LPO, NO and DPPH inhibition of 78.04%, 38.82% and 80.21% at a concentration of 1000, 125 and 500 microg/ml respectively. Oral administration of TCP (2.5, 5, 10, 20mg/kg) reduced the paw edema considerably (p<0.05) in a dose dependent manner compared to carrageenan induced rats. Similarly, oral administration of TCP (3, 10, 30 mg/kg) evoked a significant (p<0.05) dose dependent inhibitory effect on vascular permeability in mice. Altogether, these results suggest that the crude polysaccharide of T.ornata could be considered as a potential antioxidant and anti-inflammatory agent.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Biphenyl Compounds; Capillary Permeability; Carrageenan; Edema; Female; Foot; Indicators and Reagents; Lipid Peroxidation; Mice; Nitric Oxide; Nitroprusside; Oxidants; Phaeophyceae; Picrates; Polysaccharides; Rats; Rats, Sprague-Dawley; Spectroscopy, Fourier Transform Infrared; Thiobarbituric Acid Reactive Substances

The methanol extract of Russelia equisetiformis (MRE), which exhibited significant antiinflammatory activity, was evaluated for the possible mode of action by studying its antioxidant potential in adjuvant- induced arthritic rats. 1, 1 diphenyl-2-picrylhydrazyl (DPPH) radical scavenging effect was determined by spectrophotometric method. The enzymatic activity of the superoxide dismutase, glutathione peroxidase, showed a significant increase, while the lipid peroxide content was found to decrease to a large extent in MRE and indomethacin-treated rats. There was also significant and concentration-dependent increase in the percentage inhibition of DPPH, comparable to that of vitamin E and butylated hydroxyanisole (BHA) which are natural and synthetic antioxidants, respectively. The results obtained in the present study indicate that MRE possesses free radical scavenging and antioxidant properties.

Topics: Animals; Anti-Inflammatory Agents; Arthritis, Experimental; Biphenyl Compounds; Drug Evaluation, Preclinical; Edema; Female; Free Radical Scavengers; Free Radicals; Lipid Peroxides; Phytotherapy; Picrates; Plant Extracts; Rats; Rats, Wistar; Scrophulariaceae

Seven novel ferrocenic derivatives, compounds 1-7, were synthesized from steroidal drugs by Aldol condensation reaction. The derivatives were purified by chromatography, and their structures were determined on the basis of HR-ESI-MS and two-dimensional NMR spectroscopy. The purity of all derivatives was more than 95%. Compounds 1-5 demonstrated anti-proliferative activity on HeLa cell line by SRB assay more than their parent compounds. All seven derivatives showed anti-oxidative activities evaluated by DPPH scavenging and metal ion chelating, while their parent compounds gave no activity. Compound 1 indicated the most potent anti-proliferative activity similar to doxorubicin, with the GI(50) at 0.223 +/- 0.014 microg/mL. Compounds 6 and 7 demonstrated similar potent in vivo anti-inflammatory to their parent compounds (prednisolone and hydrocortisone) at 80.99 +/- 13.5 and 68.24 +/- 10.4% edema inhibition, respectively. This study has suggested that the novel compound 1 was the most potential derivative that can be further developed for cancer treatment.

Topics: Animals; Anti-Inflammatory Agents; Antineoplastic Agents; Antioxidants; Biphenyl Compounds; Drug Screening Assays, Antitumor; Edema; Ferrous Compounds; Free Radical Scavengers; HeLa Cells; Humans; Iron Chelating Agents; Magnetic Resonance Spectroscopy; Male; Metallocenes; Picrates; Rats; Rats, Sprague-Dawley; Spectrometry, Mass, Electrospray Ionization; Steroids; 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

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

Substituted hydroxycoumarins and 7- or 8-hydroxybenzo[f]coumarins were prepared by the treatment of phenols and naphthalenediols, respectively, with malic acid and H(2)SO(4) under microwave irradiation. 7- or 8-Hydroxybenzo[f]coumarins and 6-hydroxybenzo[h]coumarin were synthesized by the reaction of naphthalenediols with ethylpropiolate in the presence of ZnCl(2) in refluxing dioxane. The compounds were tested in vitro for their ability: (i) to interact with 1,1-diphenyl-2-picryl-hydrazyl (DPPH) stable free radical, (ii) to inhibit lipid peroxidation, (iii) to scavenge the superoxide anion, (iv) to inhibit the activity of soybean lipoxygenase and (v) to inhibit in vivo the carrageenin-induced rat paw edema. Most of them are potent superoxide anion scavengers and inhibit in vitro lipid peroxidation. The majority of the compounds did not show high lipoxygenase inhibitory activity. No differences were observed between biological responses of hydroxycoumarins and hydroxybenzocoumarins. Compound 3i was found to present a promising antioxidant profile.

Topics: Animals; Antioxidants; Biphenyl Compounds; Combinatorial Chemistry Techniques; Coumarins; Edema; Lipid Peroxidation; Microwaves; Molecular Structure; Picrates; Rats

Allium cepa (Family Liliaceae) is a reputed Indian medicinal herb that is prescribed as an effective remedy for several ailments in the Ayurvedic system of medicine. The aim of this study was to evaluate its efficacy against various events responsible for Type I allergic reactions. A herbal fraction (ALC-02) from A. cepa (bulb) inhibited histamine release and attenuated intracellular calcium levels in Compound 48/80-induced rat peritoneal mast cells. It also prevented Compound 48/80-mediated systemic anaphylaxis while lowering histamine levels in plasma. ALC-02 suppressed carrageenan-induced rat paw edema. It inhibited eosinophil peroxidase activity and protein content in bronchoalveolar lavage fluid (BALF) of ovalbumin-challenged mice. In this experiment ALC-02 also caused a substantial reduction in lipid peroxidation in BALF/lung tissue and augmented superoxide dismutase activity in lung tissue. ALC-02 suppressed erythrocytic lysis caused by Triton X-100. A significant quenching of 1,1-diphenyl-2-picrylhydrazyl radical by ALC-02 was observed. The results have shown a promising anti-allergic profile of ALC-02 that could be attributed to its potential antihistaminic, anti-inflammatory, and antioxidant activities.

Topics: Anaphylaxis; Animals; Anti-Allergic Agents; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Bronchoalveolar Lavage Fluid; Calcium; Edema; Eosinophil Peroxidase; Erythrocytes; Histamine; Histamine Antagonists; Lipid Peroxidation; Mast Cells; Mice; Mice, Inbred BALB C; Onions; Ovalbumin; Picrates; Plant Extracts; Plant Roots; Rats; Rats, Wistar; Superoxide Dismutase

Some new complexes of tolfenamic acid (=2-[(2-methyl-3-chlorophenyl)amino]benzoic acid; Htolf) with potentially interesting biological activities are described. The complexes [Mn(tolf)(2)(H(2)O)(2)], [Co(tolf)(2)(H(2)O)(2)], [Ni(tolf(2)(H(2)O)(2)], [Cu(tolf)(2)(H(2)O)](2), and [Zn(tolf)(2)(H(2)O)] were prepared by the reaction of tolfenamic acid, a potent anti-inflammatory drug, with metal salts. The radical-scavenging activities of the complexes were evaluated using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical-scavenging assay. Their ability to inhibit soybean lipoxygenase, beta-glucuronidase, and trypsin-induced proteolysis was studied. Their inhibitory effects on rat paw edema induced by carrageenin was studied and compared with those of tolfenamic acid. The complex [Zn(tolf)(2)(H(2)O)] exhibited the strongest in vivo inhibitory effect at 0.1 mm/kg Body Weight (BW; 93.0+/-0.9%), superior than the inhibition induced by tolfenamic acid at the same molar dose (76.0+/-0.9%). Tolfenamic acid and its metal complexes have been evaluated for antiproliferative activity in vitro against the cells of three human cancer cell lines, MCF-7 (breast cancer cell line), T24 (bladder cancer cell line), and A-549 (non-small cell lung carcinoma), and a mouse fibroblast L-929 cell line. The complexes [Mn(tolf)(2)(H(2)O)(2)] and [Cu(tolf)(2)(H(2)O)](2) have shown selectivity against T24 cell line. The IC(50) values of these two complexes against T24 cancer cell lines are in a micromolar range similar or better to that of the antitumor drug cisplatin.

Topics: Animals; Anti-Inflammatory Agents; Antineoplastic Agents; Biphenyl Compounds; Cell Line, Tumor; Drug Screening Assays, Antitumor; Edema; Free Radical Scavengers; Humans; Metals; Mice; Organometallic Compounds; ortho-Aminobenzoates; Picrates; Rats

Trioxsalen (TRX) is a 4,5',8-trimethylated psoralen analog presenting interesting biological activities when irradiated with UVA light. A series of TRX derivatives, which where obtained by its chemical modification and incorporation of a variety of unsaturated functions at position 4' of the psoralen ring-system, were evaluated for their antioxidant activity and their inhibitory activity on soybean lipoxygenase (LOX) and lipid peroxidation. The reducing properties of the compounds were evaluated using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay and found to be very low, in the range 0-14%, with the exception of the hydroxamic acid 6 which showed almost identical activity to BHT. TRX derivative 3 significantly inhibited LOX, with IC(50) 9.4 muM. With the exception of TRX, all tested analogs inhibited lipid peroxidation in the range of 35-91%. The most potent compound, namely TRX derivative 3, was studied for its anti-inflammatory activity in vivo on rat paw edema induced by carrageenan, and was found to be of almost identical activity to indomethacin. The results of the biological tests are discussed in terms of structural characteristics.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Carrageenan; Edema; Female; Free Radical Scavengers; Glycine max; Hindlimb; Indomethacin; Inflammation; Inhibitory Concentration 50; Lipid Peroxidation; Lipoxygenase; Lipoxygenase Inhibitors; Male; Picrates; Rats; Trioxsalen

Chalcones and Mannich bases have been reported to present antiinflammatory activities as well as inhibitory activities on several factors implicated in inflammation disorders. A series of chalcones and some related Mannich bases were prepared by Claisen-Schmidt condensation of appropriate acetophenones with appropriate aromatic aldehyde. Mannich bases were derived from chalcones, with formaldehyde and the corresponding amine. The compounds were tested in vitro for their ability to inhibit various enzymes involved in the arachidonic acid cascade, for their antioxidant behaviour and in vivo for anti-inflammatory activity. Some chalcones and Mannich bases present strong anti-inflammatory and antioxidant activities. Almost all the tested compounds present high inhibitory activity on lipid peroxidation. Some compounds showed potent inhibitory effect on superoxide anion formation. Among the tested compounds 5 and 6 showed the highest lipoxygenase (LO) inhibitory activity. All the tested compounds inhibit both the proteolytic and esteratic activities of trypsin and chymotrypsin. The results indicated that the anti-inflammatory effects of the compounds were partially mediated, through their antioxidant activity. Attempts to correlate quantitatively structure with activity revealed that lipophilicity and molar refractivity influence the biological response.

Topics: Anti-Inflammatory Agents, Non-Steroidal; Biphenyl Compounds; Carrageenan; Chalcones; Chymotrypsin; Edema; Esterases; Free Radical Scavengers; Glutathione; Heme; Indicators and Reagents; Lipids; Magnetic Resonance Spectroscopy; Mannich Bases; Picrates; Reactive Oxygen Species; Spectroscopy, Fourier Transform Infrared; Superoxides

The root of Carlina acanthifolia All. (Asteraceae) has been traditionally used in the treatment of various disorders including stomach and skin diseases. We studied antimicrobial, anti-inflammatory, anti-ulcer and antioxidant activities of Carlina acanthifolia root essential oil, in order to validate some of the ethnopharmacological claims. Antimicrobial activity was tested on 15 bacteria and three strains of fungi using the agar diffusion and broth microdilution methods. In assessing anti-inflammatory activity the carrageenan-induced rat paw oedema test was used, while ethanol-induced stress gastric ulcer test in rats was used in testing anti-ulcer activity. Antioxidant properties were evaluated trough the effect of the essential oil on lipid peroxidation (TBA assay) and its capability of quenching 2,2-diphenyl-1-picrylhydrazyl (DPPH) and OH radicals. The oil expressed significant antimicrobial activity, being the most active against Gram (+) bacteria: Streptococcus pyogenes, Enterococcus faecalis, Bacillus subtilis and against Candida albicans. In all applied concentrations, Carlina acanthifolia root essential oil reduced carrageenan-induced rat paw oedema in dose-dependent manner, achieving high degree of anti-inflammatory activity. The effect was comparable with that of indomethacin used as a reference drug. In the ethanol-induced stress gastric ulcer test in rats, it was shown that the tested essential oil produced significant dose-dependent gastroprotective activity. The results also pointed out substantial and dose-dependent antioxidant activity of the investigated essential oil, with carlina oxide as the main antioxidant component.

Topics: Animals; Anti-Infective Agents; Anti-Inflammatory Agents; Anti-Ulcer Agents; Antioxidants; Asteraceae; Biphenyl Compounds; Deoxyribose; Edema; Foot; Fungi; Gram-Negative Bacteria; Gram-Positive Bacteria; Hydrazines; Lipid Peroxidation; Male; Picrates; Plant Oils; Plant Roots; Rats; Rats, Wistar; Stomach Ulcer

We describe herein the discovery of LASSBio-881 (3c) as a novel in vivo antinociceptive, anti-inflammatory, and in vitro antiproliferative and antioxidant compound, with a cannabinoid ligand profile. We observed that LASSBio-881 (3c) was able to bind to CB1 receptors (71% at 100microM) and also to inhibit T-cell proliferation (66% at 10microM) probably by binding to CB2 receptors, in a non-proapoptotic manner, different from anandamide (1). It was also demonstrated that LASSBio-881 (3c) had an important antioxidant profile toward free radicals (DPPH and hydroxyl), probably due to its particular redox behavior, which reflects the presence of both nitro and 3,5-di-tert-butyl-4-hydroxyphenyl sub-units, as demonstrated by cyclic voltammetry studies. In addition, we showed that these structural sub-units are essential for the observed pharmacological activity.

Topics: Analgesics; Animals; Anti-Inflammatory Agents; Antioxidants; Arachidonic Acid; Arachidonic Acids; Biphenyl Compounds; Brain; Cannabinoid Receptor Modulators; Carrageenan; Cell Proliferation; Edema; Endocannabinoids; Female; Formaldehyde; Free Radical Scavengers; Hydrazines; Hydrazones; Ligands; Male; Mice; Models, Molecular; Pain; Picrates; Polyunsaturated Alkamides; Pyridines; Rats; Rats, Wistar; Receptor, Cannabinoid, CB1; Receptor, Cannabinoid, CB2; Structure-Activity Relationship; Superoxides; T-Lymphocytes

A series of N-substituted-quinolinone-3-aminoamides and their hybrids containing the alpha-lipoic acid functionality were designed and synthesized as potential bifunctional agents combining antioxidant and anti-inflammatory activity. The new compounds were evaluated for their antioxidant activity and for their ability to inhibit in vitro lipoxygenase as well as for their anti-inflammatory activity in vivo. In general, the derivatives were found to be potent antioxidant or anti-inflammatory agents. The results are discussed in terms of structure-activity relationships and an attempt is made to define the structural features required for activity.

Topics: Amides; Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Biphenyl Compounds; Carrageenan; Dimethyl Sulfoxide; Edema; Female; Hydrazines; Hydroxyl Radical; Lipoxygenase Inhibitors; Male; Oxidation-Reduction; Picrates; Quinolones; Rats; Rats, Inbred F344; Structure-Activity Relationship; Thioctic Acid

A series of coumarin analogs, designed and synthesised as potential fluorescent zinc probes were evaluated for their biological activity as anti-inflammatory and antioxidant agents. The effect of the synthesised compounds on inflammation, using the carrageenin-induced rat paw oedema model, was studied. In general, the compounds were found to be potent anti-inflammatory agents (26.5-64%). Compound 5 was found to interact significantly with 1,1-diphenyl-2-picryl-hydrazyl stable free radical (DPPH) whereas the remainder were inactive in this assay. The compounds inhibit in general the soybean lipoxygenase and scavenge superoxide anion radicals. The anti-inflammatory activity seems to be connected with their reducing activity. Their RM values were determined as an expression of their lipophilicity. Theoretical calculations of their lipophilicity as clog P were performed indicating that only a poor relationship exists between their lipophilicity and anti-inflammatory activity.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Biphenyl Compounds; Carrageenan; Coumarins; Drug Evaluation, Preclinical; Edema; Female; Fluorescent Dyes; Free Radical Scavengers; Glycine max; Hydrazines; Lipoxygenase; Male; Picrates; Rats; Rats, Inbred F344; Structure-Activity Relationship; Zinc

The present study was undertaken to investigate the antioxidative and antiinflammatory activities of the ethanolic extract of seeds of Torreya grandis (EST). Exposure of human dermal fibroblasts to the extract at 50 and 250 microg/ml showed significant protective effect against hydrogen peroxide (300 microM). EST not only protected cell survival from H(2)O(2)-induced toxicity, but also inhibited the H(2)O(2)-induced LDH release significantly. It was also found that EST at 100 and 1000 microg/ml showed scavenging activities of radicals and reactive oxygen species with 29.8% and 100.0% of inhibition against DPPH radical and 41.2% and 98.4% against superoxide radicals in the xanthine/xanthine oxidase system, respectively. Topically applied EST dose-dependently inhibited arachidonic acid (AA)- and 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ear edema in mice.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Arachidonic Acid; Biphenyl Compounds; Cell Survival; Dose-Response Relationship, Drug; Edema; Fibroblasts; Humans; Hydrogen Peroxide; Male; Mice; Mice, Inbred ICR; Phytotherapy; Picrates; Plant Extracts; Seeds; Superoxides; Taxaceae; Tetradecanoylphorbol Acetate

Antioxidant potential of Aspergillus candidus MTCC 2202 broth filtrate extract was studied using different antioxidant models, whereas anti-inflammatory potential was studied using carrageenan-induced rat paw oedema model. The ethyl acetate extract at 1000 microg/ml showed maximum scavenging activity of the stable radical 1,1-diphenyl,2-picryl hydrazyl upto 96.65% (IC50=430.36 microg/ml) and scavenging of the radical cation, 2,2-azinobis-(3-ethylbenzothiazoline-6-sulphonate) upto 92.25% (IC50=606.29 microg/ml) at the same concentration. The extract had good reducing power, however showed moderate inhibition for conjugated dienes and thiobarbituric acid reactive acid substances (59.56 and 51.45%). The total phenolic content of various extracts of A. candidus broth filtrate was measured and a correlation between radical scavenging activities of extracts with total phenolic content was observed. The ethyl acetate extract (125 mg/kg ip) showed significant anti-inflammatory activity in carrageenan-induced rat paw oedema model. The exhibited antioxidant activity of ethyl acetate extract of A. candidus broth filtrate was comparable with BHA and ascorbic acid, while anti-inflammatory activity was comparable with standard diclofenac sodium.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Ascorbic Acid; Aspergillus; Biphenyl Compounds; Butylated Hydroxyanisole; Cations; Culture Media; Diclofenac; Edema; Free Radicals; Hydrazines; Phenol; Picrates; Rats

Two prenylated flavanones isolated from Erythrina sigmoidea Hua (sigmoidin A and sigmoidin B) were studied for their ability to inhibit the stable 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical and arachidonic acid metabolism. In addition, the compounds were studied in two experimental models of inflammation induced in mouse ears by 12- O-tetradecanoylphorbol 13-acetate (TPA) and the phospholipase A (2)-induced mouse paw oedema. Both sigmoidins A and B proved to be potent scavengers of the DPPH radical, while the study of the inhibition of arachidonic acid metabolism demonstrated that these same compounds were selective inhibitors of 5-lipoxygenase, with no effect on cyclooxygenase-1 activity. Dose-response inhibitor potency was established for sigmoidin A (IC (50) = 31 microM). In the assay of phospholipase A (2)-induced mouse paw oedema, only the sigmoidin B derivative inhibited oedema formation at 60 min, showing a percentage of inhibition below that obtained with cyproheptadine (59 % vs. 74 %). In the TPA test, sigmoidins A and B decreased the induced oedema by 89 % and 83 %, respectively. This is the first time that the anti-inflammatory activity and antioxidant properties of these prenylflavanones have been reported. The results indicate that the compounds have different mechanisms of action depending on whether one or two prenyl groups are present in ring B.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Biphenyl Compounds; Dose-Response Relationship, Drug; Edema; Erythrina; Female; Flavanones; Flavonoids; Free Radical Scavengers; Mice; Phospholipases A; Phytotherapy; Picrates; Plant Extracts; Rats; Rats, Wistar; Tetradecanoylphorbol Acetate

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

Several thiazolyl/benzothiazolyl/benzo[d]isothiazolyl Schiff bases and hydrazones have been tested as anti-inflammatory agents and five new compounds have been synthesized. The anti-inflammatory activity was examined in vivo using the carrageenin induced mice paw edema test (inhibition 16.3-64%). The compounds were tested for antioxidant activity as hydroxyl scavengers and for their ability to interact with the stable free radical 1,1-diphenyl-2-picryl-hydrazyl (DPPH). Both anti-inflammatory and antioxidant activities depended on some structural characteristics of the synthesized compounds.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Biphenyl Compounds; Carrageenan; Chemical Phenomena; Chemistry, Physical; Dimethyl Sulfoxide; Edema; Female; Free Radical Scavengers; Hydroxyl Radical; Indicators and Reagents; Magnetic Resonance Spectroscopy; Male; Mice; Mice, Inbred AKR; Picrates; Pregnancy; Quantitative Structure-Activity Relationship; Schiff Bases; Spectrophotometry, Infrared; Thiazoles; Thiosemicarbazones

Six new iridoid glucosides, 6'-O-trans-feruloylnegundoside (1), 6'-O-trans-caffeoylnegundoside (2), 2'-O-p-hydroxybenzoyl-6'-O-trans-caffeoylgardoside (3), 2'-O-p-hydroxybenzoyl-6'-O-trans-caffeoyl-8-epiloganic acid (4), 2'-O-p-hydroxybenzoyl gardoside (5), and 2'-O-p-hydroxybenzoyl-8-epiloganic acid (6), along with two known iridoids, agnuside and negundoside, have been isolated from the ethyl acetate extractive of the leaves of Vitex altissima. The structures of these compounds were elucidated on the basis of spectral data interpretation. These isolates did not exhibit significant 5-lipoxygenase enzyme inhibitory activity, but compounds 2-4 showed potent antioxidant activity by both the superoxide (NBT riboflavin photoreduction) free-radical-scavenging and DPPH-radical-scavenging methods. Compounds 1, 2, and negundoside were evaluated in a rat paw edema assay.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Biphenyl Compounds; Edema; Enzyme Inhibitors; Free Radical Scavengers; Glucosides; India; Iridoids; Lipoxygenase Inhibitors; Molecular Structure; Picrates; Plant Leaves; Plants, Medicinal; Rats; Rats, Wistar; Vitex

Erycristagallin, a pterocarpene isolated from Erythrina mildbraedii, was tested in vitro for its antioxidant properties on the stable 2,2-diphenyl-1-pycryl-hydrazyl (DPPH) free radical and on the arachidonic acid metabolism. In addition, erycristagallin was tested on different experimental models of inflammation, such as the acute and chronic inflammation induced by the application of 12-O-tetradecanoylphorbol 13-acetate (TPA) on mice and the phospholipase A(2)-induced mouse paw oedema test. In the carrageenan-induced mouse paw oedema test, the ethyl acetate extract obtained from E. mildbraedii showed anti-inflammatory activity, and erycristagallin was isolated as the active principle. In vivo, erycristagallin significantly inhibited the phospholipase A(2)-induced mouse paw oedema as well as the mouse ear oedema induced by TPA (ID(50)<10 microg/ear). Moreover, it significantly reduced the chronic inflammation and leukocyte infiltration induced by repeated application of TPA. In vitro, erycristagallin inhibited the arachidonic acid metabolism via the 5-lipoxygenase pathway in rat polymorphonuclear leukocytes (IC(50)=23.4 microM), but had no effect on cyclooxygenase-1 metabolism in human platelets, while showing antioxidant activity in the DPPH test. As with other phenolics, the anti-inflammatory activity of erycristagallin may be based on its capacity to inhibit the arachidonic acid metabolism via the 5-lipoxygenase pathway.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Arachidonic Acid; Biphenyl Compounds; Carrageenan; Ear; Edema; Erythrina; Female; Free Radical Scavengers; Heterocyclic Compounds, 4 or More Rings; Hindlimb; Isoflavones; Leukotriene B4; Mice; Phospholipases A; Picrates; Plant Extracts; Rats; Rats, Wistar

In continuation of our previous research, several new thiazolyl/thiazolinyl/benzothiazolyl Schiff bases have been designed, synthesized and identified. The referred compounds are reported to act as lipoxygenase inhibitors affecting inflammation and/or psoriasis. The compounds were screened for their reducing activity (with the stable free radical 1,1-diphenyl-2-picryl-hydrazyl, DPPH) and for inhibition of soybean lipoxygenase (LOX). Anti-inflammatory activity was examined in vivo using the carrageenin induced mice paw edema (32.6-75%). The results are discussed in terms of structural and physicochemical characteristics of the compounds. Compound 2d possessed the highest inhibition 75%.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Edema; Hydrazines; Lipoxygenase; Lipoxygenase Inhibitors; Mice; Mice, Inbred A; Mice, Inbred AKR; Picrates; Schiff Bases; Structure-Activity Relationship

The immunomodulatory activity of the latex from Croton lechleri (sangre de drago) was determined by in vitro assays. Classical (CP) and alternative (AP) complement pathways activities were determined in human serum. Intracellular generation of reactive oxygen species (ROS) by human polymorphonuclear leukocytes (PMNs) and monocytes, and phagocytosis of opsonised fluorescent microspheres were measured by flow cytometry. Free radical scavenging activity was evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH). Activity on proliferation of murine lymphocytes was also investigated. In addition, anti-inflammatory activity was assayed in vivo by carrageenan-induced rat paw oedema test. Some of the activities were compared with those of the isolated alkaloid taspine. Sangre de drago from Croton lechleri showed immunomodulatory activity. It exhibited a potent inhibitory activity on CP and AP of complement system and inhibited the proliferation of activated T-cells. The latex showed free radical scavenging capacity. Depending on the concentration, it showed antioxidant or prooxidant properties, and stimulated or inhibited the phagocytosis. Moreover, the latex has strong anti-inflammatory activity when administered i. p. Taspine cannot be considered the main responsible for these activities, and other constituents, probably proanthocyanidins, should be also involved.

Topics: Adjuvants, Immunologic; Animals; Anti-Inflammatory Agents, Non-Steroidal; Biphenyl Compounds; Carrageenan; Complement Pathway, Alternative; Complement Pathway, Classical; Croton; Edema; Flow Cytometry; Free Radical Scavengers; Humans; Leukocytes; Mice; Phagocytosis; Phytotherapy; Picrates; Plant Oils; Rats

Four new aryl-acetic acids and the corresponding hydroxamic acids were synthesized. These compounds showed interesting interaction with the free radical 1,1-diphenyl-2-picryl-hydrazyl (DPPH), scavenging activity on .OH, inhibition of soybean lipoxygenase and a significant inhibition of carrageenin induced paw edema in rats (44.1-70.9%) at a concentration of 0.01 mmol/100 g.

Topics: Acetates; Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Biphenyl Compounds; Carrageenan; Chemical Phenomena; Chemistry, Physical; Dimethyl Sulfoxide; Edema; Free Radicals; Hydroxamic Acids; Indicators and Reagents; Lipoxygenase Inhibitors; Oxidation-Reduction; Picrates; Rats

Eight thienyl and 1,3-thiazolyl-aminoketones were synthesised and tested as anti-inflammatory agents. pKa and log P were theoretically calculated. The compounds were tested for antioxidant activity, as hydroxyl radical scavengers, as superoxide anion scavengers and for their ability to interact with 1,1-diphenyl-2-picryl hydrazyl stable free radical (DPPH). The effects of the synthesised compounds on inflammation were studied using the carrageenan induced mice paw oedema model. Both anti-inflammatory and antioxidant activities depended on some structural characteristics of the synthesised compounds.

Topics: Amines; Animals; Anti-Inflammatory Agents, Non-Steroidal; Bepridil; Biphenyl Compounds; Carrageenan; Chemical Phenomena; Chemistry, Physical; Dimethyl Sulfoxide; Edema; Female; Free Radical Scavengers; Free Radicals; Hydroxyl Radical; Ketones; Male; Mice; Mice, Inbred AKR; Picrates; Structure-Activity Relationship; Superoxides; Thiazoles; Trypsin Inhibitors

The in vitro antioxidative activities of various kinds of vinegar were investigated by using a linoleic acid autoxidation model detected by the thiobarbituric acid (TBA) method and the 1,1-diphenyl-2-picrylhydrazyl radical system. An ethyl acetate extract of Kurosu (EK), a vinegar made from unpolished rice, exhibited the highest antioxidative activity in both systems. EK (5 mg) inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced edema formation (14%) and myeloperoxidase activity (52%, P< 0.01) in female ICR mouse skin. Furthermore, EK significantly suppressed double TPA application-induced H2O2 generation (53%, P< 0.01) and lipid peroxidation determined by the TBA-reacting substance level (95 %, P< 0.01). In a two-stage carcinogenesis experiment with dimethylbenz[a]anthracene/TPA, EK significantly reduced the number of tumors per mouse by 36% (P<0.05) at 15 weeks after promotion. These results suggest that the antitumor-promoting effect may be partially due to the antioxidative properties of EK such as the decomposition of free radicals and interference with free radical-generating leukocytes.

Topics: 9,10-Dimethyl-1,2-benzanthracene; Acetic Acid; Animals; Antioxidants; Bepridil; Biphenyl Compounds; Edema; Female; Free Radical Scavengers; Free Radicals; Hydrogen Peroxide; Inflammation; Lipid Peroxidation; Mice; Mice, Inbred ICR; Oryza; Picrates; Skin; Skin Neoplasms; Tetradecanoylphorbol Acetate; Thiobarbituric Acid Reactive Substances; Time Factors; Vitamin E

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

The effect of some new 1-[3-(aroylo)] and one 1-[3-[aryloxy)]-propyl aminothiazole on inflammation was investigated in the carrageenin-induced mouse paw edema (36-58% edema inhibition). In addition they exhibited significant analgesic activity (55-80.6%) in the writhing test. Their antioxidant activity in vitro using the stable free radical 1.1-diphenyl-2-picrylhydrazyl (DPPH), was determined. Antiproteolytic ability and beta-glucuronidase inhibition have been studied. The tested compounds did not inhibit soybean 12-lipoxygenase. RM values, as an expression of lipophilicity, were determined.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Behavior, Animal; Bepridil; Biphenyl Compounds; Carrageenan; Chromatography, Thin Layer; Edema; Free Radicals; Glucuronidase; Male; Mice; Mice, Inbred AKR; Picrates; Structure-Activity Relationship; Thiazoles