Department of Organic Chemistry, Faculty of Sciences, University of Yaoundé I, Yaoundé, Cameroon.
Bioorg Med Chem Lett. 2010 Jun 15;20(12):3495-8. doi: 10.1016/j.bmcl.2010.04.145. Epub 2010 May 6.
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).
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。
