1-1-diphenyl-2-picrylhydrazyl and Stomach-Ulcer

This study aimed at investigating the gastro-protective effects of Algerian Sahara (Sidr) honey from Apis mellifera intermissa against HCl/Ethanol-induced gastric ulcers in rats.. Total phenolic content, antioxidant activity and phenolic compounds were determined. Then, three groups of rats (control, HCl/ Ethanol-induced ulcer, and orally administered honey) were used for the determination of gastro-protective effect of Sidr honey.. Total phenolic content, total flavonoid content, and DPPH activity of the honey sample were determined as 47.35±3.35 mg GAE/ 100 g, 2.13±0.17 mg QE/ 100 g, and 229.24±0.02 mg/mL, respectively. Oral pretreatment of rats with honey (1.2 g/Kg body weight orally at an interval of 2 days) protected gastric mucosa against HCl/Ethanol-induced damage by decreasing ulcer score, the volume and acidity of gastric juice and increasing pH.. These results were confirmed by the histological assessment, which demonstrated a significant gastro-protective activity of Saharian (Sidr) honey against HCl/Ethanol-induced stomach ulcer. Plasma tumor necrosis factor-α, IL-6 and PGE2 were also measured. Sahara honey significantly decreased the plasma TNF-α, PGE

Topics: Algeria; Animals; Anti-Ulcer Agents; Antioxidants; Biphenyl Compounds; Ethanol; Flavonoids; Gastric Mucosa; Honey; Hydrochloric Acid; Male; Phenols; Picrates; Plant Extracts; Protective Agents; Rats; Rats, Sprague-Dawley; Stomach Ulcer

Etlingera elatior (Jack) R.M. Smith rhizome, which has been traditionally used to reduce stomach discomfort, was reported to possess anti-inflammatory activity, however, there is a lack of such a study on the flower.. To investigate the anti-inflammatory activity of the E. elatior flower extract on gastric ulceration-induced Wistar rats. The Wistar rats were divided into 6 groups. Group 1 was the normal control, group 2 was the negative control (Arabic gum suspension 2%), group 3 was the positive control (quercetin), group 4-6 were treated with E. elatior flower extract dose of 500, 1000 and 2000 mg kg-1 of b.wt., respectively. The rats were conditioned to gastric ulceration. The stomach weight, microscopic and macroscopic evaluation of gastric mucosal damage was examined. Subsequently, the nuclear factor-kappaB-p65 (NF-kappaB-p65) expression in the fundus was Western-blotted by employing β-actin and GAPDH as the loading controls.. Etlingera elatior flower extract dose of 1000 mg kg-1 b.wt., reduces the ulceration index and the infiltration of inflammatory cells. Western blot analysis showed inhibition of NF-kappaB-p65 expression by E. elatior flower extract dose of 1000 mg kg-1 of b.wt.. Etlingera elatior flower might possess anti-inflammatory activity by downregulating the expression of NF-kappaB-p65 in the fundus of gastric ulceration-induced Wistar rats.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Biphenyl Compounds; Flowers; Gastric Mucosa; Inflammation; Inhibitory Concentration 50; Male; Phenol; Picrates; Plant Extracts; Quercetin; Rats; Rats, Wistar; Rhizome; Stomach; Stomach Ulcer; Transcription Factor RelA; Zingiberaceae

Ketoprofen belongs to one of the most common nonsteroidal anti-inflammatory drugs (NSAIDs) but its clinical usefulness has been restricted due to the high incidence of gastrointestinal complications. The release of reactive oxygen species (ROS) in NSAIDs therapy plays a major role in causing gastric complications. Antioxidants not only prevent gastric ulceration and lipid peroxidation but also preserve glutathione-type peroxidase (GPO) activity. Therefore, the present study investigates the utility of combining anti-inflammatory and antioxidant properties of two different compounds in a single molecule to form a series of 16 ketoprofen-antioxidant mutual codrugs. The free carboxylic group, which is believed to be one of the reasons for gastric toxicity of ketoprofen, was masked temporarily by simple and double esterification with alcoholic/phenolic-OH of natural antioxidants. In simple esterification, ketoprofen is directly linked to natural antioxidants (IIa-h) in the hope to obtain drugs free of gastric side effects. In an attempt to improve the in vivo lability, as well as gastric side effects, the double ester codrugs, that is, ketoprofen-antioxidant through the glycolic acid spacer (-CH

Topics: Analgesics; Animals; Anti-Inflammatory Agents, Non-Steroidal; Anti-Ulcer Agents; Antioxidants; Biphenyl Compounds; Humans; Hydrolysis; Inflammation; Ketoprofen; Kinetics; Molecular Structure; Pain; Picrates; Rats; Stomach Ulcer

Lectins are proteins able to interact specifically and reversibly with carbohydrates. They are present in all living beings, particularly in legume seeds, which have many biological functions. The aim of this study was to isolate, characterize and verify antioxidant, anti-hemolytic, antitumor and gastroprotective activities in a lectin present in seeds of Phaseolus lunatus L. var. cascavel (PLUN). The isolation of lectin was performed by size exclusion chromatography on Sephadex G-100, which was isolated from a protein capable of agglutinating only human erythrocytes type A, being this the only inhibited haemagglutination n-acetyl-d-galactosamine. Its weight was estimated by PAGE is 128kDa. The lectin is thermostable up to 80°C and is active between pH 2-11. As 8M urea was able to denature the lectin. PLUN is a glycoprotein consisting of 2% carbohydrate and has antioxidant action with ascorbic acid equivalent antioxidant capacity (μMAA/g) of 418.20, 326 and 82.9 for total antioxidant activity, ABTS radical capture and capture of DPPH radical, respectively. The lectin has antitumor activity against melanoma derived cells at doses of 100 and 50mg/ml, reducing up to 83% tumor cells, and gastroprotective action, reducing up to 63% damaged area of ​​the stomach induced by ethanol.

Topics: Acetylgalactosamine; Animals; Antineoplastic Agents, Phytogenic; Antioxidants; Benzothiazoles; Biphenyl Compounds; Cell Line, Tumor; Erythrocytes; Ethanol; Gastrointestinal Agents; Hemagglutination Tests; Humans; Male; Mice; Molecular Weight; Phaseolus; Picrates; Plant Lectins; Protein Denaturation; Seeds; Solid Phase Extraction; Stomach; Stomach Ulcer; Sulfonic Acids; Urea

Cibotium barometz is a medical herb used traditionally in the Malaysian peninsula for several ailments, including gastric ulcer. The aim of this study was assessment the anti-ulcer effects of C. barometz hair on ethanol-induced stomach hemorrhagic abrasions in animals. Seven groups of Sprague Dawley (SD) rats were administered 10% Tween 20 in the normal control and ulcer control groups, and omeprazole 20 mg/kg and 62.5, 125, 250, and 500 mg/kg of C. barometz hair extract in the experimental groups. After 60 min, the normal control group of rats was orally administered 10% Tween 20, while absolute ethanol was orally administered to the groups of ulcer control, omeprazole and experimental groups. Stomachs of the rats were examined macroscopically and histologically. Homogenates of stomachs were used to evaluate endogenous antioxidant enzyme activities.. Rats pre-fed with plant extract presented a significant decrease in the sore area, increased pH of gastric contents and preserved stomach wall mucus compared to the ulcer group. Histologically, rats pre-fed with C. barometz hair extract showed mild to moderate disruptions of the surface epithelium while animals pre-fed with absolute ethanol showed severe disruptions of the stomach epithelium with edema and leucocyte penetration of the submucosal layer. A Periodic acid Schiff (PAS) staining revealed that each rat pre-treated with the plant extract displayed an intense uptake of stomach epithelial glycoprotein magenta color compared to the ulcer control group. Immunohistochemical analysis revealed that rats pre-fed with the plant extract showed an up-regulation of the heat shock protein 70 (HSP70) and down-regulation of Bax proteins compared to ulcer control rats. Homogenates of the stomach tissue demonstrated significant increases in the endogenous antioxidant enzymatic activity and decreased lipid peroxidation (MDA) in rats pre-treated with C. barometz hair extract compared with the ulcer control rats. In acute toxicity, the liver and kidney revealed no hepatotoxic or nephrotoxic effects histologically.. The gastric cytoprotective action of C. barometz hair extract might be attributed to antioxidants, an increase in gastric pH, stomach mucus preservation, increased endogenous antioxidant enzymes, decreased lipid peroxidation, up-regulation of HSP70 and down-regulation of Bax proteins.

Topics: Animals; Antioxidants; Biphenyl Compounds; Dose-Response Relationship, Drug; Ethanol; Ferns; Male; Medicine, Chinese Traditional; Phytotherapy; Picrates; Plant Extracts; Rats; Rats, Sprague-Dawley; Stomach; Stomach Ulcer; Toxicity Tests

The present study was designed to investigate the gastroprotective effect of xanthones 7-preniljacareubin (PJB), 1,3,5,6-tetrahydroxy xanthone (THX), 3-demethyl-2-geranyl-4-prenylbellidypholine (DGP) and 1,5,8-trihydroxy-4', 5'-dimethyl-2H-pyrane (2,3:3,2)-4-(3-methylbut-2-enyl) xanthone (TDP) isolated of branches from G. achachairu. Their structures were identified through the spectroscopic analysis in comparison with previously reported data. The xanthones were tested at dose of 10 mg/kg against ethanol 60%/HCl 0.3 N-induced gastric ulcer in female swiss mice. The xanthones PJB, THX, DGP and TDP exhibit gastroprotective effect after intraperitoneal treatment, but only the first two displayed anti-ulcer activity after oral administration. Both PJB and THX augmented the antioxidative capacity of tissue by an increase in glutathione levels, as well as were able to prevent an increase in myeloperoxidase activity and tumor necrosis factor level. On the other hand, only THX showed an in vitro free radical scavenger activity, and only PJB avoided mucus depletion on gastric mucosa, which was not associated with an increase in mucin production at glandular level. In addition, PJB and THX inhibited the in vitro H(+)K(+)-ATPase activity at similar range as omeprazole. Together, these results demonstrate the anti-ulcer efficacy of xanthones isolated from G. achachairu, which can contribute for future directions in the development of effective strategies to improve gastric diseases.

Topics: Animals; Anti-Ulcer Agents; Antioxidants; Biphenyl Compounds; Carbon-13 Magnetic Resonance Spectroscopy; Female; Free Radical Scavengers; Garcinia; Gastric Mucosa; Glutathione; H(+)-K(+)-Exchanging ATPase; Immunohistochemistry; Inflammation; Mice; Mucins; Peroxidase; Picrates; Protective Agents; Proton Magnetic Resonance Spectroscopy; Stomach Ulcer; Tumor Necrosis Factor-alpha; Xanthones

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

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

In traditional medicine, the leaves, flowers, barks and roots of Muntingia calabura L. (Muntingiaceae) have been employed as a treatment for various ailments including dyspepsia and to relieve pain caused by gastritis and peptic ulcer disease. The methanolic extract of Muntingia calabura leaves (MEMC) has been proven in the previous study to possess significant antiulcer activity. In this study, we attempted to determine the prophylactic effect of the fractions obtained from MEMC against ethanol-induced gastric lesion in rats and the involvement of antioxidants and anti-inflammatory mediators.. The MEMC was fractionated with petroleum ether (PEF), ethyl acetate (EAF) and distilled water (AQF). These fractions were investigated for possible antiulcer property using ethanol-induced gastric ulcer rat model. The rats were administered orally once daily with 8% Tween 80 (control), 100mg/kg ranitidine, or the fractions, in the doses of 100, 250, and 500 mg/kg, for 7 days, followed by ulcer induction using absolute ethanol. The rats were euthanized; macroscopic and histological observations of the stomach were done. The ulcer area (UA) was determined and the percentage protection afforded by the fractions was calculated. The fractions were subjected to antioxidant studies including the superoxide and 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging, oxygen radical absorbance capacity (ORAC) and total phenolic content (TPC) assay. Involvement of nitric oxide (NO) and inflammatory mediators such as lipoxygenase (LOX) and xanthine oxidase (XO) were evaluated. Phytochemical screening and HPLC analysis of the fractions were also conducted.. Pre-treatment of PEF and EAF significantly (p<0.001) attenuated the gastric lesions as compared to the control group in a dose-dependent manner. On the other hand, 100 and 250 mg/kg of AQF significantly (p<0.001) prevented the ulcer formation but at the highest dose (500 mg/kg), AQF failed to significantly reduce the ulcer formation, showing a dose-independent antiulcerative effect of AQF. The histological evaluation supported the observed gastroprotective activity of PEF, EAF and AQF. All the fractions showed high superoxide and DPPH scavenging activity, meanwhile the EAF showed highest TPC followed by PEF and AQF. These fractions also significantly (p<0.05) inhibited the NO while maintaining the viability of the cells. EAF exhibited high inhibition towards both the LOX and XO enzymes, meanwhile PEF and AQF exerted high LOX inhibition but low XO inhibition. Phytochemical screening and HPLC profiling suggested the presence of flavonoid- and tannin based compounds in PEF and EAF.. It can be concluded that the prophylactic effect of the fractions on gastric ulceration in rats is associated with its high antioxidant activity and its ability to effectively inhibit the inflammation mediators. Presence of several flavonoids and gallic acid explains the effectiveness of the fractions in affording protection against gastric damages.

Topics: Animals; Anti-Inflammatory Agents; Anti-Ulcer Agents; Antioxidants; Biphenyl Compounds; Cell Line; Cell Survival; Ethanol; Magnoliopsida; Male; Methanol; Mice; Nitrites; Phytotherapy; Picrates; Plant Extracts; Plant Leaves; Rats, Sprague-Dawley; Solvents; Stomach Ulcer; Superoxides; Xanthine Oxidase

In this study, we evaluated the gastric protective activities of mokdanpi in vitro. Further, we used experimental ulcer models to identify the active ingredients of mokdanpi. As a preliminary evaluation of mokdanpi ethanolic extract and its ingredients, we assessed its radical scavenging activities. In addition, its antimicrobial activity against Helicobacter pylori (H. pylori) was investigated. The antiulcerogenic activity of the active ingredients was evaluated in pylorus-ligated rats, an HCl/ethanol-induced and an absolute ethanol-induced ulcer model. We confirmed the scavenging effect of the ethanolic extract of mokdanpi and its ingredients against 2,2-diphenyl-1-picrylhydrazyl, nitric oxide and superoxide radicals, and we demonstrated that mokdanpi could inhibit the colonization of H. pylori. In an HCl-ethanol-induced ulcer model, gallic acid and catechin (100 mg/kg) inhibited 40.6% and 41.7% of gastric lesions, respectively. Catechin (100 mg/kg) significantly reduced (p<0.05) the gastric secretion induced by pylorus ligature in rats in comparison to the control group. Gallic acid (100 mg/kg) significantly increased (p<0.05) the mucus contents in an ethanol-induced ulcer model. The antioxidant ingredients (catechin and gallic acid) present in mokdanpi play a major role in antiulcerogenic activity, and demonstrate novel activity against H. pylori.

Topics: Animals; Anti-Infective Agents; Anti-Ulcer Agents; Antioxidants; Biphenyl Compounds; Catechin; Ethanol; Gallic Acid; Gastric Juice; Gastric Mucosa; Helicobacter pylori; Ligation; Mucus; Nitric Oxide; Paeonia; Phytotherapy; Picrates; Plant Extracts; Plant Roots; Rats; Rats, Sprague-Dawley; Stomach Ulcer; Superoxides

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

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

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

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

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

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

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

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

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

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

Opuntia ficus indica f. inermis methanolic root extract (ORE) was investigated for phenolic and flavonoids contents, in vitro evaluated for DPPH radical scavenging activity, reducing power and in vivo tested for its gastro-protective ability against 80% ethanol induced ulcer in rats. Phytochemical test of ORE were positive for phenolic and flavonoid contents. DPPH radical scavenging activity and reducing power of ORE showed an EC(50) of 118.65±2.51 μg/ml and 300 μg/ml respectively. In vivo the pre-treatment of rats with ranitidine (50 mg/kg) and 200, 400, and 800 mg/kg doses of ORE significantly (p<0.05) reduced the 80% ethanol induced-ulcer lesion, with a rate of 82.68%, 49.21%, 83.13%, and 92.59% respectively, and prevented the depletion of antioxidant enzymes, superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), total glutathione (GSH), and inhibited the increase of myeloperoxidase (MPO) and malondialdehyde (MDA) in rat stomach tissues when compared with ethanol group. Also pre-treatment with ORE marked a dose-dependent attenuation of histopathology changes induced by ethanol. Phenolic and flavonoids wealth, radical scavenging activity, and reducing power, have been implicated for antiulcer property of ORE.

Topics: Animals; Anti-Ulcer Agents; Antioxidants; Biphenyl Compounds; Dose-Response Relationship, Drug; Flavonoids; Male; Malondialdehyde; Opuntia; Peroxidase; Phenols; Phytotherapy; Picrates; Plant Extracts; Plant Roots; Polyphenols; Ranitidine; Rats; Rats, Wistar; Stomach; Stomach Ulcer

Leaf fractions of Wilbrandia ebracteata were investigated for anti-ulcerogenic effects in ethanol and indomethacin-induced gastric ulcer assays in mice. Protective anti-ulcer effects were detected only in the ethanol-induced ulcer assay effects after pre-treatment with MeOH extract, MeOH chlorophyll-free, chlorophyll residue, HEX, DCM, aqueous MeOH fraction, ethyl acetate (EtOAc) and aqueous fractions. A potent anti-ulcerogenic effect was determined after pre-treatment of animals with EtOAc fraction, which was fractionated for isolation of active constituents. Seven flavonoids, 3',4',5,6,7,8-hexahydroxyflavonol, orientin, isoorientin, vitexin, isovitexin, luteolin, 6-methoxi-luteolin were isolated from the leaves of W. ebracteata (Cucurbitaceae) by chromatographic methods and identified by their spectral data. The data suggest that flavonoids are active anti-ulcerogenic compounds from leaves of W. ebracteata. The ability of scavenging free radicals was evaluated by DPPH reduction assay by TLC of flavonoids isolated.

Topics: Administration, Oral; Animals; Anti-Ulcer Agents; Biphenyl Compounds; Brazil; Cucurbitaceae; Flavonoids; Indomethacin; Mice; Picrates; Plant Extracts; Plant Leaves; Plants, Medicinal; Stomach Ulcer

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

The gastroprotective activity of the diterpene ferruginol isolated from Prumnopitys andina wood and bark was determined on HCl/EtOH-induced gastric lesions in mice. The effect of the compound on the healing of subacute gastric lesions in rats was also studied. The mode of action of the diterpene was assessed using human gastric epithelial cells (AGS) and MRC-5 fibroblasts. The effect of ferruginol on the prostaglandin E2 content, protection against sodium taurocholate induced-damage and reduced glutathione content was evaluated on AGS cells as well as on the growth of AGS and fibroblast cultures. The free radical scavenging effect of ferruginol was assessed by the 1,1-diphenyl-2-picryl-hydrazil radical and superoxide anion assays. The effect of ferruginol on human erythrocyte membrane lipoperoxidation was determined. The cytotoxicity of the compound was assessed by means of the neutral red uptake. At 25 mg/kg, ferruginol inhibited the appearance of gastric lesions by 60% showing similar effects than lansoprazole at 20 mg/kg. Additionally, the compound displayed a significant ulcer healing activity in rats at 25 and 50 mg/kg with curative ratios of 36.0% and 92.5%, respectively, while the reference compound ranitidine at 50 mg/kg showed a curative ratio of 79.6%. At 6 and 12 microM, ferruginol increased significantly the prostaglandin E2 content. A strong inhibition of lipoperoxidation was found (IC50: 1.4 microM), but no effect was observed on the sodium taurocholate induced-damage or reduced glutathione content. Ferruginol stimulated cell proliferation at 1-2 microM in AGS cells and at 4-8 microM in fibroblasts, with cytotoxicities (IC50) of 24 and 26 microM, respectively. Our results support that ferruginol acts as gastroprotective increasing the PGs content, protecting the cells against lipid peroxidation and improving the gastric ulcer healing by a stimulating effect on the cell proliferation. These findings encourage further pharmacological studies of ferruginol as a potential new anti-ulcerogenic drug.

Topics: Abietanes; Acetic Acid; Animals; Anti-Ulcer Agents; Biphenyl Compounds; Cell Line; Cell Survival; Dinoprostone; Diterpenes; Epithelial Cells; Erythrocyte Membrane; Ethanol; Fibroblasts; Free Radical Scavengers; Gastric Mucosa; Glutathione; Hydrochloric Acid; Lipid Peroxidation; Male; Mice; Oxidation-Reduction; Picrates; Ranitidine; Rats; Rats, Sprague-Dawley; Solvents; Stomach Ulcer; Superoxides; Taurocholic Acid