Effects of nitro-heterocyclic derivatives against Leishmania (Leishmania) infantum promastigotes and intracellular amastigotes
Exp. parasitol
; 163: 68-75, Apr. 2016. ilus, tab
Artigo
em Inglês
| Sec. Est. Saúde SP, SESSP-IIERPROD, Sec. Est. Saúde SP
| ID: biblio-1021080
Biblioteca responsável:
BR31.1
Localização: BR31.1; 2016_P-003
ABSTRACT
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
Texto completo:
Disponível
Coleções:
Bases de dados nacionais
/
Brasil
Base de dados:
Sec. Est. Saúde SP
/
SESSP-IIERPROD
Assunto principal:
Leishmania infantum
/
Compostos Heterocíclicos
Idioma:
Inglês
Revista:
Exp. parasitol
Ano de publicação:
2016
Tipo de documento:
Artigo
Instituição/País de afiliação:
Secretaria de Estado da Saúde. São Paulo/BR
/
Universidade de São Paulo/BR