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Pathog Glob Health ; 106(2): 107-12, 2012 May.
Article in English | MEDLINE | ID: mdl-22943546

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.


Subject(s)
Antiprotozoal Agents/pharmacology , Benzoates/pharmacology , Camphanes/pharmacology , Trypanosoma cruzi/drug effects , Animals , Antiprotozoal Agents/chemical synthesis , Antiprotozoal Agents/toxicity , Benzoates/chemical synthesis , Benzoates/toxicity , Camphanes/chemical synthesis , Camphanes/toxicity , Cell Survival/drug effects , Cytoplasm/ultrastructure , Hep G2 Cells , Humans , Inhibitory Concentration 50 , Macrophages, Peritoneal/drug effects , Macrophages, Peritoneal/parasitology , Mice , Mice, Inbred BALB C , Trypanosoma cruzi/growth & development , Trypanosoma cruzi/ultrastructure
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