| Author | Soares, Milena Botelho Pereira | |
| Author | Silva, Cinara Vasconcelos da | |
| Author | Bastos, Tanira Matutino | |
| Author | Guimarães, Elisalva Teixeira | |
| Author | Figueira, Cláudio Pereira | |
| Author | Smirlis, Despina | |
| Author | Azevedo Junior, Walter Filgueira de | |
| Access date | 2014-08-11T19:30:51Z | |
| Available date | 2014-08-11T19:30:51Z | |
| Document date | 2012 | |
| Citation | SOARES, M. B. P. et al. Anti-Trypanosoma cruzi activity of nicotinamide. Acta Tropica, v. 122, n. 2, p. 224– 229, 2012. | pt_BR |
| ISSN | 0001-706X | |
| URI | https://www.arca.fiocruz.br/handle/icict/8186 | |
| Language | eng | pt_BR |
| Publisher | Elsevier Science B.V | pt_BR |
| Rights | open access | pt_BR |
| Title | Anti-Trypanosoma cruzi activity of nicotinamide | pt_BR |
| Type | Article | pt_BR |
| DOI | 10.1016/j.actatropica.2012.01.001 | |
| 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. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, Brasil | pt_BR |
| Affilliation | Laboratory of Molecular Parasitology, Microbiology. Dpt, Hellenic Pasteur Institute. Athens, Greece | pt_BR |
| Affilliation | 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 | pt_BR |
| Subject | Sirtuin | pt_BR |
| Subject | Trypanosoma cruzi | pt_BR |
| Subject | Nicotinamide | pt_BR |
| Subject | Virtual screening | pt_BR |
