Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/8186
Title: Anti-Trypanosoma cruzi activity of nicotinamide
Authors: Soares, Milena Botelho Pereira
Silva, Cinara Vasconcelos da
Bastos, Tanira Matutino
Guimarães, Elisalva Teixeira
Figueira, Cláudio Pereira
Smirlis, Despina
Azevedo Junior, Walter Filgueira de
Affilliation: Fundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, Brasil
Fundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, Brasil
Laboratory of Molecular Parasitology, Microbiology. Dpt, Hellenic Pasteur Institute. Athens, Greece
Pontifícia Universidade Católica do Rio Grande do Sul – PUCRS. Faculdade de Biociências. Instituto Nacional de Ciência e Tecnologia em Tuberculose-CNPq. Laboratório de Bioquímica Estrutural. Porto Alegre, RS, Brasil / Pontifícia Universidade Católica do Rio Grande do Sul. Porto Alegre, RS, Brasil
Abstract: Inhibition of Trypanosoma brucei and Leishmania spp. sirtuins has shown promising antiparasitic activity, indicating that these enzymes may be used as targets for drug discovery against trypanosomatid infections. In the present work we carried out a virtual screening focused on the C pocket of Sir2 from Trypanosoma cruzi. Using this approach, the best ligand found was nicotinamide. In vitro tests confirmed the anti-T. cruzi activity of nicotinamide on epimastigote and trypomastigote forms. Moreover, treatment of T. cruzi-infected macrophages with nicotinamide caused a significant reduction in the number of amastigotes. In addition, alterations in the mitochondria and an increase in the vacuolization in the cytoplasm were observed in epimastigotes treated with nicotinamide. Analysis of the complex of Sir2 and nicotinamide revealed the details of the possible ligand–target interaction. Our data reveal a potential use of TcSir2 as a target for anti-T. cruzi drug discovery.
Keywords: Sirtuin
Trypanosoma cruzi
Nicotinamide
Virtual screening
Issue Date: 2012
Publisher: Elsevier Science B.V
Citation: SOARES, M. B. P. et al. Anti-Trypanosoma cruzi activity of nicotinamide. Acta Tropica, v. 122, n. 2, p. 224– 229, 2012.
DOI: 10.1016/j.actatropica.2012.01.001
ISSN: 0001-706X
Copyright: open access
Appears in Collections:BA - IGM - Artigos de Periódicos

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