Trypanocidal Activity of Triterpenes from Arrabidaea triplinervia and Derivatives(Pharmacognosy)

概要

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Ethanol extract from Arrabidaea triplinervia leaves showed in vitro activity (ED_<100> 5.0mg/ml) against trypomastigotes of Trypanosoma cruzi, the etiologic agent of Chagas disease. Bioactivity-directed fractionation of this extract led to the isolation of ursolic and oleanolic acids as trypanocidal compounds besides pomolic acid (not tested) and alpinetine (inactive). A series of natural and synthetic derivatives of ursolic and oleanolic acids was simultaneously assayed for structure activity relationships (SAR) studies. Ursolic acid (ED_<100> 0.4mg/ml) was four times more active than oleanolic acid (ED_<100> 1.6mg/ml). The presence of free hydroxy and/or carboxy groups is necessary for the trypanocidal activity as could be deduced from the effect of the acetates, methyl ester, and aldehyde derivatives.
公益社団法人日本薬学会の論文
2006-11-01