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

Experimental Parasitology
Simone Carolina Soares Petri e SilvaJosé Angelo Lauletta Lindoso

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 show...Continue Reading

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Citations

May 28, 2019·The Journal of Venomous Animals and Toxins Including Tropical Diseases·Daiane Barros Dias MendonçaJose Angelo Lauletta Lindoso
Nov 4, 2020·Drug Development Research·Christina KannigaduDavid D N'Da
Jan 23, 2021·RSC Medicinal Chemistry·Sushobhan MukhopadhyaySanjay Batra

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