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可乐果中柯拉维龙对啮齿动物的抗溃疡和质子泵(H⁺,K⁺ -ATP酶)抑制活性

Anti-ulcerogenic and proton pump (H+, K+ ATPase) inhibitory activity of Kolaviron from Garcinia kola Heckel in rodents.

作者信息

Onasanwo Samuel A, Singh Neetu, Olaleye Samuel B, Palit Gautam

机构信息

Department of Physiology, Faculty of Basic Medical Sciences, College of Medicine, University of Ibadan, Ibadan, Nigeria.

出版信息

Indian J Exp Biol. 2011 Jun;49(6):461-8.

PMID:21702226
Abstract

Anti-ulcer potential and proton pump inhibitory activity of kolaviron (KV) isolated from Garcinia kola Heckel has been evaluated using different ulcer models. Cold-restraint (CRU), aspirin (ASP), alcohol (AL), pyloric ligation (PL) induced gastric ulcer models were used to assess anti-ulcerogenic activity of KV in rats. Effects of KV on gastric juice for free and total acidity, peptic activity and mucin secretion were also evaluated. The H+, K+-ATPase activity was assayed in gastric microsomes, spectrophotometrically. Results of this study showed that KV (200 mg/kg) reduced the incidence of ulcers in CRU (69.0%), PL (67.6%), ASP (68.6%) and AL (51.5%). Reductions were also observed in free acidity (32.6%), total acidity (56.2%) and peptic activity (35.4%) with increase in mucin secretion by 40.1%. KV inhibited the H+,K+-ATPase activity with IC50 of 43.8 microg/ml compared with omeprazole with IC50 of 32.3 microg/ml. KV showed both cytoprotective and anti-secretory potentials against peptic ulcer models, and a proton pump inhibitory activity. KV may emerge as a potent anti-ulcer compound.

摘要

从可乐果( Garcinia kola Heckel)中分离出的可乐维酮(KV)的抗溃疡潜力和质子泵抑制活性已通过不同的溃疡模型进行了评估。采用冷束缚(CRU)、阿司匹林(ASP)、乙醇(AL)、幽门结扎(PL)诱导的胃溃疡模型来评估KV对大鼠的抗溃疡活性。还评估了KV对胃液游离酸度、总酸度、胃蛋白酶活性和黏液分泌的影响。采用分光光度法测定胃微粒体中的H +,K + -ATP酶活性。本研究结果表明,KV(200 mg/kg)降低了CRU(69.0%)、PL(67.6%)、ASP(68.6%)和AL(51.5%)模型中溃疡的发生率。游离酸度(32.6%)、总酸度(56.2%)和胃蛋白酶活性(35.4%)也有所降低,黏液分泌增加了40.1%。KV抑制H +,K + -ATP酶活性,IC50为43.8μg/ml,而奥美拉唑的IC50为32.3μg/ml。KV对消化性溃疡模型显示出细胞保护和抗分泌潜力以及质子泵抑制活性。KV可能成为一种有效的抗溃疡化合物。

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