Anti-ulcer compound from Voacanga africana with possible histamine H2 receptor blocking activity

Anti-ulcer compound from Voacanga africana with possible histamine H2 receptor blocking activity
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DOI:
10.1016/s0944-7113(00)80037-9
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发表时间:
2000-12-01
期刊:
影响因子:
7.9
通讯作者:
Nyasse, B
Nyasse, B
中科院分区:
医学1区
文献类型:
--
作者:
Tan, PV;Nyasse, B

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Voacanga africana在喀麦隆民族医学中用于治疗消化性溃疡。我们已经测试了从果实提取物中获得的生物碱(TN)的细胞保护,抗分泌和溃疡愈合作用。TN(50-100 mg/kg)对盐酸/乙醇(36- 75%)、无水乙醇(43- 75%)、盐酸-乙醇/吲哚美辛(58- 84%)、幽门结扎(31- 100%)、冷束缚应激(68- 100%)和组胺(49- 100%)引起的溃疡形成有剂量依赖性的预防作用。吲哚美辛(20 mg/kg,i. p.)预处理未抑制50和100 mg/kg对HCl/乙醇的抑制作用。TN将Shay结扎的胃酸分泌从对照组的77 mEq/l降低至50酸100 mg/kg剂量的46和25 mEq/l。增加组胺诱导的胃酸分泌从对照组的84 mEq/l降低至两种剂量TN的45和21 mEq/l,50 mg/kg剂量完全抑制胃溃疡和十二指肠溃疡。与对照组相比,50和100 mg/kg剂量的TN对慢性乙酸诱导的溃疡的愈合率分别为62%和83%。TN具有类似于组胺受体阻滞剂的胃抗分泌作用。其细胞保护和溃疡愈合特性与其通过增强胃粘液产生来加强胃粘膜防御的能力有关。
Voacanga africana is used in Cameroonian ethnomedicine for the treatment of peptic ulcers. We have tested the cytoprotective, anti-secretory and ulcer healing actions of an alkaloid (TN) obtained from the fruit extract. Oral administration of TN (50-100 mg/kg) dose-dependently prevented ulcer formation by HCl/ethanol (36-75 %), absolute ethanol (43-75 %), HCl-ethanol/indomethacin (58-84 %), Pylorus ligation (31-100 %), cold restraint stress (68-100 %) and histamine (49-100 %). The inhibitory effect at 50 and 100 mg/kg against HCl/ethanol was not suppressed by pre-treatment with indomethacin (20 mg/kg, i.p.). TN reduced Shay-ligated gastric acid secretion from 77 mEq/l in the controls to 46 and 25 mEq/l for the 50 acid 100 mg/kg doses. Augmented histamine-induced gastric acid secretion was reduced from 84 mEq/l in the controls to 45 and 21 mEq/l for the two doses of TN, with total inhibition of gastric and duodenal ulcers by the 50 mg/kg dose. Healing rate of chronic acetic acid-induced ulcers was 62 and 83 %, respectively, for the dose of 50 and 100 mg/kg of TN compared with the controls. TN has gastric anti-secretory effects similar to histamine receptor blockers. Its cytoprotective and ulcer healing properties are related to its ability to strengthen gastric mucosal defenses through enhanced gastric mucus production.