phytosterols and Stomach-Ulcer

Geographically the prevalence of duodenal ulceration is related to the staple foods in the diet in regions of developing countries where the diet is stable. It is higher in regions where the diet is based on milled rice, refined wheat or maize, yams, cassava, sweet potato, or green bananas, and is lower in regions where the staple diet is based on unrefined wheat or maize, soya, certain millets or certain pulses. Experiments on rat gastric and duodenal ulcer models showed that it was the lipid fraction in staple foods from low prevalence areas that was protective against both gastric and duodenal ulceration, including ulceration due to non-steroidal anti-inflammatory drugs (NSAIDs). It also promoted ulcer healing. The lipid from the pulse, Dolichos biflorus, horse gram which was highly protective was used to identify the fractions with protective activity in the lipid. The protective activity lay in the phospholipid, sterol and sterol ester fractions. In the phospholipid fraction phosphatidyl choline (lethicin) and phosphatidyl ethanolamine (cephalin) were predominant. In the sterol fraction the sub-fractions showing protective activity contained β-sitosterol, stigmasterol, and an unidentified isomer of β-sitosterol. The evidence from animal models shows that certain dietary phospholipids and phytosterols have a protective action against gastroduodenal ulceration, both singly and in combination. This supports the protective role of staple diets in areas of low duodenal ulcer prevalence and may prove to be of importance in the prevention and treatment of duodenal ulceration and management of recurrent ulcers. A combination of phospholipids and phytosterols could also play an important role in protection against ulceration due to NSAIDs.

Topics: Animals; Cytoprotection; Diet; Dietary Fats; Dietary Fiber; Disease Models, Animal; Duodenal Ulcer; Duodenum; Gastric Mucosa; Phospholipids; Phytosterols; Plant Oils; Rats; Stomach; Stomach Ulcer

Gorgonians of the genus Eunicella are known for possessing a wide range of pharmacological activities such as antiproliferative and antibacterial effect. The aim of this study was to evaluate the anti-inflammatory and gastroprotective effect of the organic extract and its semi-purified fractions from the white gorgonian Eunicella singularis and the isolation and identification of pure compound(s) from the more effective fraction.. Anti-inflammatory activity was evaluated, using the carrageenan-induced rat paw edema test and in comparison to the reference drug Acetylsalicylate of Lysine. The gastroprotective activity was determined using HCl/EtOH induced gastric ulcers in rats. The purification of compound(s) from the more effective fraction was done by two chromatographic methods (HPLC and MPLC). The structure elucidation was determined by extensive spectroscopic analysis (1H and 13C NMR, COSY, HMBC, HMQC and NOESY) and by comparison with data reported in the literature.. The evaluation of the anti-inflammatory activity of different fractions from Eunicella singularis showed in a dependent dose manner an important anti-inflammatory activity of the ethanol fraction, the percentage of inhibition of edema, 3 h after carrageenan injection was 66.12%, more effective than the reference drug (56.32%). In addition, this ethanolic fraction showed an interesting gastroprotective effect compared to the reference drugs, ranitidine and omeprazol. The percentage of inhibition of gastric ulcer induced by HCl/ethanol in rats was 70.27%. The percentage of the reference drugs (ranitidine and omeprazol) were 65 and 87.53%, respectively. The purification and structure elucidation of compound(s) from this ethanolic fraction were leading to the isolation of five sterols: cholesterol (5α-cholest-5-en-3β-ol) (1); ergosterol (ergosta-5,22-dien-3β-ol) (2); stigmasterol (24-ethylcholesta-5,22-dien-3b-ol) (3); 5α,8α-epidioxyergosta 6,22-dien-3β-ol (4) and 3β-hydroxy-5α,8α-epidioxyergosta-6-ene (5); and one diterpenoid: palmonine D (6).. Based on data presented here, we concluded that diterpenoids and sterols detected in the ethanolic fraction can be responsible for its pharmacological activity.

Topics: Animals; Anthozoa; Anti-Inflammatory Agents; Anti-Ulcer Agents; Carrageenan; Disease Models, Animal; Diterpenes; Drug Discovery; Edema; Ethanol; Female; Hydrochloric Acid; Male; Phytosterols; Rats; Rats, Wistar; Stomach Ulcer

Gastric ulcer is an illness that affects a great number of people worldwide. The goal of the present research was to assess the anti-ulcerogenic activity of nymphayol (NYM), isolated from Nymphaea stellata, against an ethanol-induced ulcer model in rats. Administration of ethanol elevates the levels of the ulcer index (UI) along with causing tremendous increases in lipid peroxidation and myeloperoxidase (MPO) and significant decreases in gastric mucus, catalase (CAT), superoxide dismutase (SOD), glutathione (GSH), glutathione peroxidase (GPx), and prostaglandin E2 (PGE2). However, the NYM- (45 mg/kg) pretreated animals showed considerable increases in antioxidants, gastric mucus, and PGE2 level and significant decreases in UI, lipid peroxidation, and MPO level. Pro-inflammatory cytokines such as interleukin-6 (IL-6), interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α), and interferon-γ (IFN-γ) were increased and the level of interleukin-10 (IL-10), an anti-inflammatory cytokine, was decreased in ethanol-induced ulcerated animals, and these inequalities were amended by NYM pretreatment. Pro-apoptotic markers including caspase-8, caspase-9, and caspase-3 were decreased and Bcl-2, an anti-apoptotic marker, was increased through NYM pretreatment, as compared with the ethanol-induced ulcer group. Pretreatment with indomethacin, SC560, rofecoxib, and Nω-Nitro-L-arginine methyl ester (L-NAME) considerably prevented the ulcer protective activity of NYM (45 mg/kg), indicating the involvement of cyclooxygenase (COX) and nitric oxide synthase (NOS) in NYM-mediated gastroprotection against ethanol-induced ulcer. These outcomes suggest that the gastroprotective effect of NYM might be mediated by adjustment of inflammatory mediators and apoptotic markers and increasing antioxidants.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Apoptosis; Dose-Response Relationship, Drug; Ethanol; Female; Flowers; Male; Molecular Conformation; Nymphaea; Phytosterols; Rats; Rats, Wistar; Stomach Ulcer; Structure-Activity Relationship

Blepharis maderaspatensis L. Roth (BM) (Acanthaceae) and Ammannia baccifera L. (AB) (Lythraceae) are used in folk medicine for various stomach disorders.. The chloroform and ethanol extracts of both plants were evaluated for antioxidant, gastric antisecretory, and gastroprotective properties.. Antioxidant properties of the extracts were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and nitric oxide (NO) scavenging assay. The gastric antisecretory properties of the extracts were assessed, at a dose of 100 and 200 mg/kg, using aspirin-pylorus ligation induced gastric ulcer models and the gastroprotective activity of the extracts was assessed, at a dose of 100 and 200 mg/kg, using HCl-ethanol induced ulcer models in rats.. Ethanol extract of BM (EBM) possessed good antioxidant property with IC₅₀ values of 37.4 and 44.1 µg/mL in DPPH and NO scavenging assays respectively, where 25-250 µg/mL concentration in DPPH assay and 30-300 µg/mL concentration in NO scavenging assay were used. Ethanol extract of AB (EAB) at a dose of 200 mg/kg reduced the free acidity to 142.66 mEq/L and total acidity to 451.22 mEq/L. It reduced the gastric secretion with increase in pH from 2.2 to 3.15. Possessing good antisecretory activity, it also reduced the ulcer by 92.2% in aspirin and pylorus ligation induced gastric ulcer models. EAB increased the mucus secretion and adherent mucus in the tissues with a 71.43% reduction of ulcerin HCl-ethanol induced ulcer models, at a dose of 200 mg/kg. This activity can be attributed to the various flavonoids like rutin and kaempferol-3-O-β-glucopyranoside, and the phytosterol, β-sitosterol-3-O-β-glucopyranoside, and phenolics present in the extracts.. EBM possessed significant antioxidant property while EAB possessed good antisecretory and gastroprotective activity.

Topics: Acanthaceae; Adhesiveness; Animals; Anti-Ulcer Agents; Ethnopharmacology; Female; Flavonoids; Free Radical Scavengers; Gastric Acid; Gastric Mucosa; India; Lythraceae; Male; Mucus; Phytosterols; Phytotherapy; Plant Extracts; Plant Leaves; Rats; Rats, Wistar; Stomach Ulcer; Toxicity Tests, Acute

'Marjoram,' Origanum majorana L., a culinary aromatic medicinal herb is known to possess various therapeutic properties. We evaluated the antiulcerogenic activity of the ethanol extract in hypothermic restraint stress-, indomethacin-, necrotizing agents- (80% ethanol, 25% NaCl and 0.2 M NaOH) induced ulcers and basal gastric acid secretion using pylorus ligated Shay rat-model. Marjoram at doses of 250 and 500 mg/kg of body weight, significantly decreased the incidence of ulcers, basal gastric secretion and acid output. Furthermore, the extract replenished the ethanol-induced depleted gastric wall mucus and nonprotein sulfhydryls (NP-SH) contents and significantly lowered the increase in the concentration of malondialdehyde (MDA). Ulcer preventing potential was further confirmed by histopathological assessment. An acute toxicity test showed a large margin of safety of the extract in mice. The phytochemical screening of aerial parts of marjoram revealed the presence of volatile oil, flavonoids, tannins, sterols and/or triterpenes.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Disease Models, Animal; Drugs, Chinese Herbal; Female; Gastric Acid; Gastric Mucosa; Indomethacin; Male; Malondialdehyde; Mice; Oils, Volatile; Origanum; Phytosterols; Rats; Stomach Ulcer; Sulfhydryl Compounds; Tannins; Triterpenes

In order to investigate the effect of cycloartenol ferulic acid ester (CFE, CAS 21238-33-5), a component of gamma-oryzanol which is a phytosterol derived from rice bran, on the central nervous system, a variety of pharmacological tests were performed. It was shown that CFE had a suppressant effect on the central nervous system, but its properties were different from those of existing major and minor tranquilizers. In addition, its efficacy in several models of cerebral dysfunction was demonstrated. Since any clear effects could not be obtained under the treatments with gamma-oryzanol, CFE seems to be more useful than gamma-oryzanol. Thus the results of this study suggest that CFE may serve as a new plant-derived cerebral activator possessing a wide range of pharmacological actions.

Topics: Amnesia; Animals; Anticonvulsants; Avoidance Learning; Blood Pressure; Body Temperature; Cats; Central Nervous System; Circadian Rhythm; Coma; Conflict, Psychological; Coumaric Acids; Female; Hypolipidemic Agents; Male; Mice; Mice, Inbred ICR; Motor Activity; Oryza; Pentobarbital; Phytosterols; Rats; Rats, Wistar; Reserpine; Sleep; Stomach Ulcer