Effects of nitro-heterocyclic derivatives against Leishmania (Leishmania) infantum promastigotes and intracellular amastigotes

Autor(es)

Soares Petri e Silva, Simone Carolina ^[1] ; Palace-Berl, Fanny ^[2] ; Tavares, Leoberto Costa ^[2] ; Castro Soares, Sandra Regina ^[1] ; Lauletta Lindoso, Jose Angelo ^{[1, 3, 4]}

Afiliação do(s) autor(es)

^[1] Univ Sao Paulo, Inst Trop Med, Lab Soroepidemiol & Imunobiol, BR-05508 Sao Paulo - Brazil

^[2] Univ Sao Paulo, Fac Ciencias Farmaceut, Lab Planejamento Desenvolvimento Farmacos, BR-05508 Sao Paulo - Brazil

^[3] Secretaria Estado Saude Sao Paulo, Inst Infectol Emilio Ribas, Sao Paulo - Brazil

^[4] Lab Soroepidemiol LIM 38 HC FMUSP, Sao Paulo - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Experimental Parasitology; v. 163, p. 68-75, APR 2016.
• Citações Web of Science: 4

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 MIT 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. (C) 2016 Elsevier Inc. All rights reserved. (AU)

• Processo FAPESP: 14/06061-4 - Nitrocompostos com atividade em Trypanosoma cruzi: planejamento, síntese, avaliação da citotoxicidade e bioatividade in vitro e estudos de relações estrutura-atividade in silico
• Beneficiário: Leoberto Costa Tavares
• Modalidade de apoio: Auxílio à Pesquisa - Regular