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Exp Parasitol ; 163: 68-75, 2016 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-26795261

RESUMO

Leishmaniasis is an overlooked tropical disease affecting approximately 1 million people in several countries. Clinical manifestation depends on the interaction between Leishmania and the host's immune response. Currently available treatment options for leishmaniasis are limited and induce severe side effects. In this research, we tested nitro-heterocyclic compounds (BSF series) as a new alternative against Leishmania. Its activity was measured in Leishmania (Leishmania) infantum promastigotes and intracellular amastigotes using MTT colorimetric assay. Additionally, we assessed the phosphatidylserine exposure by promastigotes, measured by flow cytometry, as well as nitric oxide production, measured by Griess' method. The nitro-heterocyclic compounds (BSF series) showed activity against L. (L.) infantum promastigotes, inducting the phosphatidylserine exposition by promastigotes, decreasing intracellular amastigotes and increasing oxide nitric production. The selectivity index was more prominent to Leishmania than to macrophages. Compared to amphotericin b, our compounds presented higher IC50, however the selectivity index was more specific to parasite than to amphotericin b. In conclusion, these nitro-heterocyclic compounds showed to be promising as an anti-Leishmania drug, in in vitro studies.


Assuntos
Antiprotozoários/farmacologia , Compostos Heterocíclicos/farmacologia , Leishmania infantum/efeitos dos fármacos , Leishmaniose Visceral/tratamento farmacológico , Nitrocompostos/farmacologia , Antiprotozoários/química , Antiprotozoários/uso terapêutico , Apoptose , Linhagem Celular , Relação Dose-Resposta a Droga , Citometria de Fluxo , Compostos Heterocíclicos/química , Compostos Heterocíclicos/uso terapêutico , Humanos , Concentração Inibidora 50 , Leishmania infantum/crescimento & desenvolvimento , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Macrófagos/parasitologia , Monócitos/efeitos dos fármacos , Óxido Nítrico/metabolismo , Nitrocompostos/química , Nitrocompostos/uso terapêutico , Fosfatidilserinas/análise
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