Antimicrobial activity of synthetic bornyl benzoates against Trypanosoma cruzi

作者:Correa P R C; Miranda R R S; Duarte L P; Silva G D F; Vieira Filho S A; Okuma A A; Carazza F; Morgado Diaz J A; Pinge Filho P; Yamauchi L M; Nakamura C V; Yamada Ogatta S F*
来源:Pathogens and Global Health, 2012, 106(2): 107-112.
DOI:10.1179/2047773212Y.0000000002

摘要

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%26apos;,4%26apos;,5%26apos;-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 ICs50/72h of two synthetic L-bornyl benzoates, 1 and 2, was 10.1 and 12.8 mu g/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.

  • 出版日期2012-5