Anti-Trypanosoma cruzi activity of nicotinamide

Detalhes bibliográficos
Autor(a) principal: Soares, Milena Botelho Pereira
Data de Publicação: 2012
Outros Autores: Silva, Cinara Vasconcelos da, Bastos, Tanira Matutino, Guimarães, Elisalva Teixeira, Figueira, Cláudio Pereira, Smirlis, Despina, Azevedo Junior, Walter Filgueira de
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/8186
Resumo: Fundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, Brasil
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spelling Soares, Milena Botelho PereiraSilva, Cinara Vasconcelos daBastos, Tanira MatutinoGuimarães, Elisalva TeixeiraFigueira, Cláudio PereiraSmirlis, DespinaAzevedo Junior, Walter Filgueira de2014-08-11T19:30:51Z2014-08-11T19:30:51Z2012SOARES, M. B. P. et al. Anti-Trypanosoma cruzi activity of nicotinamide. Acta Tropica, v. 122, n. 2, p. 224– 229, 2012.0001-706Xhttps://www.arca.fiocruz.br/handle/icict/818610.1016/j.actatropica.2012.01.001engElsevier Science B.VAnti-Trypanosoma cruzi activity of nicotinamideinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleFundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, BrasilFundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, BrasilFundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, BrasilFundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, BrasilFundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, BrasilLaboratory of Molecular Parasitology, Microbiology. Dpt, Hellenic Pasteur Institute. Athens, GreecePontifícia 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, BrasilInhibition 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.SirtuinTrypanosoma cruziNicotinamideVirtual screeninginfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZORIGINALSoares MB Anti-Trypanosoma....pdfSoares MB Anti-Trypanosoma....pdfapplication/pdf1207763https://www.arca.fiocruz.br/bitstream/icict/8186/1/Soares%20MB%20Anti-Trypanosoma....pdf69f837370e5c46f7e1843460c2bd4154MD51LICENSElicense.txtlicense.txttext/plain; charset=utf-81914https://www.arca.fiocruz.br/bitstream/icict/8186/2/license.txt7d48279ffeed55da8dfe2f8e81f3b81fMD52TEXTSoares MB Anti-Trypanosoma....pdf.txtSoares MB Anti-Trypanosoma....pdf.txtExtracted texttext/plain31880https://www.arca.fiocruz.br/bitstream/icict/8186/3/Soares%20MB%20Anti-Trypanosoma....pdf.txtaf132c77a40ef61af26efcc7f1e5aab2MD53icict/81862023-03-15 14:32:55.637oai:www.arca.fiocruz.br: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ório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352023-03-15T17:32:55Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false
dc.title.pt_BR.fl_str_mv Anti-Trypanosoma cruzi activity of nicotinamide
title Anti-Trypanosoma cruzi activity of nicotinamide
spellingShingle Anti-Trypanosoma cruzi activity of nicotinamide
Soares, Milena Botelho Pereira
Sirtuin
Trypanosoma cruzi
Nicotinamide
Virtual screening
title_short Anti-Trypanosoma cruzi activity of nicotinamide
title_full Anti-Trypanosoma cruzi activity of nicotinamide
title_fullStr Anti-Trypanosoma cruzi activity of nicotinamide
title_full_unstemmed Anti-Trypanosoma cruzi activity of nicotinamide
title_sort Anti-Trypanosoma cruzi activity of nicotinamide
author Soares, Milena Botelho Pereira
author_facet Soares, Milena Botelho Pereira
Silva, Cinara Vasconcelos da
Bastos, Tanira Matutino
Guimarães, Elisalva Teixeira
Figueira, Cláudio Pereira
Smirlis, Despina
Azevedo Junior, Walter Filgueira de
author_role author
author2 Silva, Cinara Vasconcelos da
Bastos, Tanira Matutino
Guimarães, Elisalva Teixeira
Figueira, Cláudio Pereira
Smirlis, Despina
Azevedo Junior, Walter Filgueira de
author2_role author
author
author
author
author
author
dc.contributor.author.fl_str_mv Soares, Milena Botelho Pereira
Silva, Cinara Vasconcelos da
Bastos, Tanira Matutino
Guimarães, Elisalva Teixeira
Figueira, Cláudio Pereira
Smirlis, Despina
Azevedo Junior, Walter Filgueira de
dc.subject.en.pt_BR.fl_str_mv Sirtuin
Trypanosoma cruzi
Nicotinamide
Virtual screening
topic Sirtuin
Trypanosoma cruzi
Nicotinamide
Virtual screening
description Fundação Oswaldo Cruz. Centro de Pesquisa Gonçalo Moniz. Salvador, BA, Brasil
publishDate 2012
dc.date.issued.fl_str_mv 2012
dc.date.accessioned.fl_str_mv 2014-08-11T19:30:51Z
dc.date.available.fl_str_mv 2014-08-11T19:30:51Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.citation.fl_str_mv SOARES, M. B. P. et al. Anti-Trypanosoma cruzi activity of nicotinamide. Acta Tropica, v. 122, n. 2, p. 224– 229, 2012.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/8186
dc.identifier.issn.none.fl_str_mv 0001-706X
dc.identifier.doi.none.fl_str_mv 10.1016/j.actatropica.2012.01.001
identifier_str_mv SOARES, M. B. P. et al. Anti-Trypanosoma cruzi activity of nicotinamide. Acta Tropica, v. 122, n. 2, p. 224– 229, 2012.
0001-706X
10.1016/j.actatropica.2012.01.001
url https://www.arca.fiocruz.br/handle/icict/8186
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Elsevier Science B.V
publisher.none.fl_str_mv Elsevier Science B.V
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
instname:Fundação Oswaldo Cruz (FIOCRUZ)
instacron:FIOCRUZ
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