Trypanocidal Activity of Pimarane Diterpenes from Viguiera arenaria (Asteraceae)

被引：33

作者：

Ambrosio, Sergio R. ^{[2
]}

Arakawa, Nilton S. ^{[1
]}

Esperandim, Viviane R. ^{[3
]}

de Albuquerque, Sergio ^{[3
]}

Da Costa, Fernando B. ^{[1
]}

机构：

[1] Univ Sao Paulo, Fac Ciencias Farmaceut, Dept Ciencias Farmaceut, Lab Farmacognosia, BR-14040903 Ribeirao Preto, SP, Brazil

[2] Univ Sao Paulo, Fac Filosofia Ciencias & Letras Ribeirao Pret, Dept Quim, BR-14040903 Ribeirao Preto, SP, Brazil

[3] Univ Sao Paulo, FCFRP, Dept Anal Clin, BR-14040903 Ribeirao Preto, SP, Brazil

来源：

PHYTOTHERAPY RESEARCH | 2008年 / 22卷 / 10期

基金：

巴西圣保罗研究基金会;

关键词：

Asteraceae; pimarane diterpenes; trypanocidal activity; Viguiera arenaria;

D O I：

10.1002/ptr.2512

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Five structurally related pimarane diterpenes isolated from the roots of Viguiera arenaria and a further compound obtained by chemical derivatization were evaluated in vitro against the trypomastigote forms of Trypanosoma cruzi. The natural compound ent-15-pimarene-8 beta,19-diol and the derivative ent-8(14),15-pimaradiene-3 beta-acetoxy showed the highest trypanocidal activity, displaying IC50 values of 116.5 +/- 1.21 and 149.3 +/- 1.07 mu M, respectively, while the positive control, violet gentian, showed an IC50 of 76 mu M. Based on the results, it can be concluded that minor structural differences among the tested diterpenes influence significantly the trypanocidal activity, thus bringing new perspectives to the establishment of structure-activity relationships among this type of metabolites to the treatment of Chagas' disease. Copyright (C) 2008 John Wiley & Sons, Ltd.

引用

页码：1413 / 1415

页数：3

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