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

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art_SILVA_Effects_of_nitroheterocyclic_derivatives_against_Leishmania_Leishmania_infantum_2016.PDF (1.48 MB)
Citações na Scopus
14
Tipo de produção
article
Data de publicação
2016
DOI
Scopus
Web of Science
PubMed
Título da Revista
ISSN da Revista
Título do Volume
Editora
ACADEMIC PRESS INC ELSEVIER SCIENCE
Autores
PALACE-BERL, Fanny
TAVARES, Leoberto Costa
Citação
EXPERIMENTAL PARASITOLOGY, v.163, p.68-75, 2016
Projetos de Pesquisa
Unidades Organizacionais
Fascículo
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.
Palavras-chave
Leishmania (L.) infantum, Nitroheterocyclic compounds, THP-1 cells, Nitric oxide, Apoptosis
URI
https://observatorio.fm.usp.br/handle/OPI/14585
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Coleções
Artigos e Materiais de Revistas Científicas - LIM/38