A novel icetexane diterpene, 5-epi-icetexone from Salvia gilliessi is active against Trypanosoma cruzi.

Abstract:

:In this work the effect of a novel compound, 5-epi-icetexone (ICTX) obtained from Salvia gilliessi Benth. (Labiatae), is studied on cultured epimastigotes of Trypanosoma cruzi (Tulahuen). It was found that the compound exerts an antiproliferative effect on the parasites at concentrations between 2.8 and 4.2 microM, and similar sensitivity in other strains (Dm28c, CL-Brener and Y-strain). The compound was deleterious at concentrations higher than 4.2 microM, with an estimated IC50 of 6.5+/-0.75 microM, but with low cytotoxicity to mammalian cells. These effects were irreversible, even at short times of exposure to the drug. In solution, ICTX showed to be stable for at least 96 h at 29 degrees C. With cytostatic dose a little percentage of parasites was resistant to the action of ICTX, and they continued growing although with different kinetic. By electron transmission microscopy, at dose of 4.2 microM an external vesiculization was observed on the first day of exposure to the compound, but the parasite cytoplasm became plenty of vacuoles and exhibited nuclear disorganization from the second day of exposure. It was concluded that ICTX is active against T. cruzi and may act by multiple mechanisms. In future, this novel icetexane diterpene may be a good candidate for therapeutic use against Chagas' disease.

journal_name

Acta Trop

journal_title

Acta tropica

authors

Sanchez AM,Jimenez-Ortiz V,Sartor T,Tonn CE,García EE,Nieto M,Burgos MH,Sosa MA

doi

10.1016/j.actatropica.2005.12.007

subject

Has Abstract

pub_date

2006-05-01 00:00:00

pages

118-24

issue

2

eissn

0001-706X

issn

1873-6254

pii

S0001-706X(06)00045-3

journal_volume

98

pub_type

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