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Evaluation of inhibitory potential of l. amazonensis efflux pumps by furoxan derivative 14e

Grant number: 15/17911-1
Support type:Scholarships in Brazil - Scientific Initiation
Effective date (Start): February 01, 2016
Effective date (End): July 31, 2017
Field of knowledge:Biological Sciences - Parasitology
Principal Investigator:Marcia Aparecida Silva Graminha
Grantee:Jéssica Naiara Varonez da Fonseca
Home Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil

Abstract

A novel series of furoxan have been recently synthesized, characterized, and evaluated for in vitro activity against promastigote and intracellular amastigote forms of Leishmania amazonensis. The furoxan derivatives exhibited the ability to generate nitric oxide at different levels (7.8% to 27.4%) and showed remarkable leishmanicidal activity against both promastigote and intracellular amastigote forms. The main goal of this proposal is to evaluate the hypothesis that 14e is able to inhibit efflux pumps in L. amazonenensis through flow cytometry using promastigotes cells (wild type and resistant to 14e) stained with rhodamine 123, a well-known substrate for efflux pumps. If 14e is able to inhibit these membrane proteins, we expect the accumulation in cells of rhodamine123. We will also evaluate the ability of 14e to improve the antileishmanial activity of amphotericin B (check board analysis).