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Planta Med ; 75(12): 1336-8, 2009 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-19431103

RESUMO

Isocordoin (1) and 2',4'-dihydroxy-3'-(gamma,gamma-dimethylallyl)-dihydrochalcone (7), chalcones isolated from the root of Lonchocarpus xuul, together with six analogues of 1 were tested in vitro against promastigotes of Leishmania mexicana and epimastigotes of Trypanosoma cruzi. Additionally, cytotoxic studies with MDCK cells were carried out using the MTT method. Among these derivatives, 2',4'-diacetoxy-3'-(3-methylbut-2-enyl)-chalcone (2) and 2',4'-dimethoxy-3'-(3-methylbut-2-enyl)-chalcone (3) showed the strongest antiprotozoal activity and lower cytotoxicity in comparison with isocordoin at a concentration in the microM range. Derivative 3 had the strongest trypanocidal activity with IC(50) values lower than those of nifurtimox and benznidazole, the common drugs used against these parasites. The selectivity index calculated for 3 (SI 109.3) confirms the selective trypanocidal activity of this metabolite.


Assuntos
Antiprotozoários/farmacologia , Catecóis/farmacologia , Fabaceae/química , Leishmania mexicana/efeitos dos fármacos , Trypanosoma cruzi/efeitos dos fármacos , Animais , Antiprotozoários/química , Antiprotozoários/isolamento & purificação , Ascomicetos , Catecóis/química , Catecóis/isolamento & purificação , Linhagem Celular , Cães , Concentração Inibidora 50 , Extratos Vegetais/química
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