Antiulcer Activity

A bilberry extract containing 25% anthocyanidins (Myrtocyan) demonstrated antiulcer activity in several rat models (5). Efficacy was measured using an "index of ulceration" and means were compared using the MannWhitney U test. Minimum doses producing statistically significant benefit were 100 mg/kg for ulcers induced by pyloric ligation, 25 mg/kg for reser-pine ulcer, and 100 mg/kg for phenylbutazone ulcers (p < 0.01 compared to control). For acetic acid ulcers, efficacy was determined by measuring the ulcer surface area. The minimum effective dose was 50 mg/kg (p < 0.01 compared to control, Dunnett t-test). For restraint ulcer, efficacy was determined by comparing the number of ulcers in the control vs bilberry groups. The minimum effective dose was 100 mg/kg (p < 0.01 compared with control, Mann-Whitney U-test). Effects on volume or pH of gastric secretion were ruled out as a mechanism of action. Histological examination of the gastric mucosa showed increased mucus production in treated rats. Bilberry's beneficial effects were attributed to an increase in production of mucopolysaccharides.

Based on the promising results of this study, the antiulcer activity of the individual anthocyanidins was studied. One anthocyanidin, 3,5,7-trihydroxy-2-(3,4-dihydroxyphenyl)-1-benzopyrylium chloride (IdB 1027, Inverni della Beffa S.p.A., Milan) showed particular promise, and so it was produced synthetically so that its effects on several animal models of acute and chronic stomach ulcers could be studied further (4). IdB 1027 administrered orally or intraperitoneally was able to inhibit acute gastric ulceration induced by pyloric ligation, stress (cold plus restraint), phenylbutazone, indometha-cin, reserpine, ethanol, and histamine, as well as duodenal ulceration induced by cysteamine and chronic gastric ulcers induced by acetic acid. Results of additional experiments suggest the mechanism of action involves stimulation of protective gastric mucosal secretions. A drawback of this study is that the severity of ulceration caused by phenylbutazone, indomethacin, ethanol, and histamine was assessed using nonvalidated ordinal scales.

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