4.5 Article

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

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 12, 页码 3495-3498

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.04.145

关键词

Annonaceae; Polyalthia suaveolens; Alkaloids; Trypanosomatidae; Glycolysis; Inhibition

资金

  1. European Commission [ICA4-CT-2001-10075]

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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 mu M) 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). Crown Copyright (C) 2010 Published by Elsevier Ltd. All rights reserved.

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