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从使君子科使君子属植物光叶丁子香中的抗锥虫生物碱:对三种布氏锥虫糖酵解酶的影响。

Antitrypanosomal alkaloids from Polyalthia suaveolens (Annonaceae): their effects on three selected glycolytic enzymes of Trypanosoma brucei.

机构信息

Department of Organic Chemistry, Faculty of Sciences, University of Yaoundé I, Yaoundé, Cameroon.

出版信息

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3495-8. doi: 10.1016/j.bmcl.2010.04.145. Epub 2010 May 6.

Abstract

In continuation of our study on medicinal plants of Cameroon, stem barks of Polyalthia suaveolens were phytochemically studied. This investigation yielded a new indolosesquiterpene alkaloid, named polysin (1) and four hitherto known alkaloids (2-5). Polysin (1) appeared as a competitive reversible inhibitor (K(i)=10 microM) of phosphofructo kinase (PFK) of Trypanosoma brucei with respect to fructose-6-phosphate (K(i)/K(M)=0.05) and could be used in the design of new trypanocidal drugs. The other isolated compounds (2-5) also exhibited interesting inhibitory effects on selected glycolytic enzymes (PFK, glyceraldehyde-3-phosphate dehydrogenase and aldolase).

摘要

在我们对喀麦隆药用植物的研究中,对软叶波罗蜜的茎皮进行了植物化学研究。这项研究产生了一种新的吲哚倍半萜生物碱,命名为 polysin(1)和四种以前已知的生物碱(2-5)。Polysin(1)表现为对布氏锥虫磷酸果糖激酶(PFK)相对于果糖-6-磷酸(K(i)/ K(M)=0.05)的竞争性可逆抑制剂(K(i)=10 microM),可用于设计新的杀锥虫药物。其他分离出的化合物(2-5)也对选定的糖酵解酶(PFK、甘油醛-3-磷酸脱氢酶和醛缩酶)表现出有趣的抑制作用。

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