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Bioorg Med Chem Lett ; 26(7): 1772-5, 2016 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-26906638

RESUMO

Six plant metabolites including isobavachalcone (1), 4-hydroxylonchocarpine (2), and (E)-1-(2,2-dimethyl-2H-chromen-6-yl)-3-(4-hydroxyphenyl)prop-2-en-1-one (3), 6,8-(di-3-methyl-but-2-enyl)eriodictyol (4), damnacanthal (5), and buesgenine (6) were evaluated for their leishmanicidal and trypanocidal activities against intracellular amastigotes of Leishmania amazonensis and Trypanosoma cruzi. Compounds 2-4 and 6 displayed antileishmanial activity while 3 and 5 showed trypanocidal effect. The leishmanicidal activity of 6 was expressed with the lowest IC50 (5.70µg/mL) whereas the most trypanocidal metabolite (5) showed its activity with IC50 at 11.14µg/mL. In addition, antiprotozoal effect of mixtures of 1-6 prepared at different ratios (3:1, 1:1, and 1:3) was also investigated. Interestingly, 1 and 2 initially inactive against T. cruzi, displayed trypanocidal activities when mixed together. This activity increased when 3 (13.63µg/mL) was combined with 1 in ratios 1:1 (10.01µg/mL) and 3:1 (7.78µg/mL). Moreover, the leishmanicidal effect of 4 against L. amazonensis increased in the mixture 6/4 (1:3).


Assuntos
Antiparasitários/química , Antiparasitários/farmacologia , Leishmania mexicana/efeitos dos fármacos , Plantas/química , Trypanosoma cruzi/efeitos dos fármacos , Alcaloides/química , Alcaloides/farmacologia , Antraquinonas/química , Antraquinonas/farmacologia , Antiprotozoários/química , Antiprotozoários/farmacologia , Doença de Chagas/tratamento farmacológico , Chalconas/química , Chalconas/farmacologia , Flavanonas/química , Flavanonas/farmacologia , Humanos , Leishmaniose Cutânea/tratamento farmacológico , Moraceae/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Rubiaceae/química , Relação Estrutura-Atividade , Tripanossomicidas/química , Tripanossomicidas/farmacologia , Zanthoxylum/química
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