Trypanocidal activity of triterpenes from Arrabidaea triplinervia and derivatives.
Biol Pharm Bull
; 29(11): 2307-9, 2006 Nov.
Article
em En
| MEDLINE
| ID: mdl-17077535
ABSTRACT
Ethanol extract from Arrabidaea triplinervia leaves showed in vitro activity (ED100 5.0 mg/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 (ED100 0.4 mg/ml) was four times more active than oleanolic acid (ED100 1.6 mg/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.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Triterpenos
/
Tripanossomicidas
/
Bignoniaceae
Limite:
Animals
Idioma:
En
Revista:
Biol Pharm Bull
Assunto da revista:
BIOQUIMICA
/
FARMACOLOGIA
Ano de publicação:
2006
Tipo de documento:
Article
País de afiliação:
Brasil