Abstract
American trypanosomiasis (Chagas disease) continues to be a significant public health problem, and the therapeutic potential of current antichagasic agents (nifurtimox and benznidazole) is rather limited. Here we report on the antitrypanosomal effect of 1-methoxyspirobrassinol and other indole phytoalexins--secondary metabolites produced by Cruciferous plants. These compounds, that previously demonstrated antimicrobial and anticancer properties, displayed significant antiproliferative effects on intracellular amastigotes of Trypanosoma cruzi and may be prospective candidates for antichagasic drug design and development.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antiprotozoal Agents / pharmacology*
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Drug Evaluation, Preclinical
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Indoles / chemistry
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Indoles / pharmacology*
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Inhibitory Concentration 50
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Myoblasts / drug effects
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Myoblasts / parasitology
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Phytoalexins
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Rats
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Sesquiterpenes
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Spiro Compounds / chemistry
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Spiro Compounds / pharmacology
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Structure-Activity Relationship
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Terpenes / pharmacology*
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Thiazoles / chemistry
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Thiazoles / pharmacology
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Thiocarbamates / chemistry
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Thiocarbamates / pharmacology
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Trypanosoma cruzi / drug effects*
Substances
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1-methoxyspirobrassinin
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Antiprotozoal Agents
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Indoles
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Sesquiterpenes
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Spiro Compounds
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Terpenes
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Thiazoles
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Thiocarbamates
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spirobrassinin
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brassinin
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Phytoalexins