Methyl angolensate (1), the major compound isolated from the methanol extract of the stem bark of Entandrophragma angolense produced a dose-related inhibition of gastric ulceration, 40 mg/kg body weight (B.W.) being more effective than 40 mg/kg B.W. of propranolol. The highest dose used (80 mg/kg B.W.) completely inhibited gastric ulceration and significantly reduced gastric acidity (P < 0.05). Furthermore, 1 (40 mg/kg B.W.) significantly reduced gastric acid secretion induced by histamine (1.0 mg/kg B.W.) and carbachol (1.0 mg/kg B.W.). These results suggest that 1 produces its antiulcer activity by inhibition of gastric acid secretion.

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Background and Objectives: Medicinal plants are the richest, cheapest and most readily available source of drugs, nutraceuticals and food supplements. Pharmaceutical industries still rely largely on medicinal plants for intermediates due to their chemical diversities. This study, therefore, investigated the chemical constituents, thermal decomposition products and biological activities of extract from seeds of Cola nitida (the 'kola nut').

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Diarrhea is a prevalent gastrointestinal problem associated with fatal implications. It is a huge public health concern that requires better alternatives to current drugs. This study investigated the mechanisms involved in the antidiarrheal activity of Anacardium occidentale (Ao) stem bark extract, a plant commonly used in the management of diarrhea in Nigeria. Methanolic stem bark extract of the plant was partitioned into three fractions: hexane fraction, ethyl acetate fraction (AoEF) and methanol fraction. In vitro studies on the effect of these fractions on guinea pig ileum (GPI) strips, as well as the modulatory effect of AoEF on standard agonists- and antagonists-induced GPI contraction and relaxation, revealed AoEF as the most active fraction. In vivo studies to assess the effect of AoEF on the dopaminergic, muscarinic, and serotonergic pathways were carried out using gastric emptying (GE) and gastrointestinal transit (GT) as experimental end points. AoEF was subjected to GC-MS analysis, while the identified compounds were docked with the muscarinic acetylcholine receptor M3 (CHRM3) using AutodockVina. Results indicated that AoEF inhibited GE and GT via inhibition of CHRM3. In addition, GC-MS analysis revealed the presence of 24 compounds in AoEF, while docking indicated that octadecanoic acid 2-(2-hydroxylethoxy) ethyl ester exhibited the highest binding affinity to CHRM3. This study indicated that the antidiarrheal activity of Ao is through its antimotility effect via the inhibition of the muscarinic pathway. And since none of the identified compounds exhibited higher binding affinity to CHRM3 relative to loperamide, the antimotility activity of these phytoconstituents may be via synergism.

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The effect of a methanol extract of the stem bark of Entandrophragma angolense was investigated on indomethacin-induced gastric ulcer in rats. The effect of the extract was dose-dependent, doses ranging from 0.4 to 1.6 g/kg produced significant effect (p<0.05). At the highest dose used (1.6 g/kg) complete inhibition of ulceration occurred. The probable mechanism of action of E . angolense is discussed.

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