Antimicrobial activity of synthetic bornyl benzoates against Trypanosoma cruzi

Abstract

We report here for the first time the in vitro effects of (1S,2R,4S)-1,7,7-trimethyl-bicyclo[2·2·1]heptan-2-yl-3′,4′,5′-trimethoxy benzoate (1) and (1S,2R,4S)-1,7,7-trimethyl-bicyclo[2·2·1]heptan-2-yl benzoate (2) on the growth and ultrastructure of Trypanosoma cruzi. These two synthetic compounds exerted an antiproliferative effect on the epimastigote forms of the parasite. The ICs_50/72h of two synthetic L-bornyl benzoates, 1 and 2, was 10·1 and 12·8 μg/ml, respectively. Both compounds were more selective against epimastigotes than HEp-2 cells. Ultrastructural analysis revealed intense cytoplasmic vacuolization and the appearance of cytoplasmic materials surrounded by membranes. The treatment of peritoneal macrophages with compounds 1 and 2 caused a significant decrease in the number of T. cruzi-infected cells. L-Bornyl benzoate derivatives may serve as a potential source for the development of more effective and safer chemotherapeutic agents against T. cruzi infections.

Keywords:

• Antimicrobial activity
• L-Bornyl benzoate
• Trypanosoma cruzi

This study was supported by grants from DECIT/SCTIE/MS and MCT by Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), Programa de Núcleos de Excelência (PRONEX/Fundação Araucária), and Programa de Pós-Graduação em Microbiologia da Universidade Estadual de Londrina. We thank Dr A. Leyva for reading this manuscript. This work is part of the MSc dissertation of P. R. C. Corrêa.