Trypanosoma cruzi: antiproliferative effect of indole phytoalexins on intracellular amastigotes in vitro.
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.
Mezencev
Roman
R
Georgia Institute of Technology, School of Biology, Cherry Emerson Building, 310 Ferst Drive, Atlanta, GA 30332, USA. rmezencev3@gatech.edu
Galizzi
Melina
M
Kutschy
Peter
P
Docampo
Roberto
R
D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D032446:Myoblasts / Q000187:drug effects / Q000469:parasitology; D051381:Rats; D012717:Sesquiterpenes; D013141:Spiro Compounds / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013729:Terpenes / Q000494:pharmacology*; D013844:Thiazoles / Q000737:chemistry / Q000494:pharmacology; D013859:Thiocarbamates / Q000737:chemistry / Q000494:pharmacology; D014349:Trypanosoma cruzi / Q000187:drug effects*; D000094162:Phytoalexins
C497735:1-methoxyspirobrassinin; D000981:Antiprotozoal Agents; D007211:Indoles; D012717:Sesquiterpenes; D013141:Spiro Compounds; D013729:Terpenes; D013844:Thiazoles; D013859:Thiocarbamates; C417935:spirobrassinin; C089020:brassinin; D000094162:Phytoalexins