Antileishmanial activity of lapachol analogues

Detalhes bibliográficos
Autor(a) principal: Lima, Nadja M. F.
Data de Publicação: 2004
Outros Autores: Correia, Clariane S., Leon, Leonor L., Machado, Gérzia M. C., Madeira, Maria de Fátima, Santana, Antônio Euzébio G., Goulart, Marília O. F.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/33447
Resumo: Maria de Fátima Madeira. Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Documento produzido em parceria ou por autor vinculado à Fiocruz, mas não consta a informação no documento.
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spelling Lima, Nadja M. F.Correia, Clariane S.Leon, Leonor L.Machado, Gérzia M. C.Madeira, Maria de FátimaSantana, Antônio Euzébio G.Goulart, Marília O. F.2019-06-10T19:57:18Z2019-06-10T19:57:18Z2004LIMA, Nadja M. F. et al. Antileishmanial activity of lapachol analogues. Memórias do Instituto Oswaldo Cruz, Rio de Janeiro, v. 99, n. 7, p. 757-761, Nov. 2004.0074-0276https://www.arca.fiocruz.br/handle/icict/3344710.1590/S0074-027620040007000171678-8060Maria de Fátima Madeira. Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Documento produzido em parceria ou por autor vinculado à Fiocruz, mas não consta a informação no documento.Universidade Federal de Alagoas. Centro de Ciências Exatas e Naturais. Departamento de Química. Maceió, AL, Brasil.Universidade Federal de Alagoas. Centro de Ciências Exatas e Naturais. Departamento de Química. Maceió, AL, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Departamento de Imunologia. Rio de Janeiro, RJ, Brasil.Universidade Federal de Alagoas. Centro de Ciências Exatas e Naturais. Departamento de Química. Maceió, AL, Brasil.Universidade Federal de Alagoas. Centro de Ciências Exatas e Naturais. Departamento de Química. Maceió, AL, Brasil.The antileishmanial activity of lapachol, isolapachol, and dihydrolapachol, along with soluble derivatives (potassium salt) and acetate was obtained. All the compounds were assayed against metacyclic promastigotes of two different species of Leishmania associated to tegumentar leishmaniasis: L. amazonensis and L. braziliensis. All compounds presented significant activity, being isolapachol acetate the most active against promastigotes, with IC50/24h = 1.6 ± 0.0 µg/ml and 3.4 ± 0.5 µg/ml for, respectively, L. amazonensis and L. braziliensis. This compound was also assayed in vivo against L. amazonensis and showed to be active. Its toxicity in vitro was also established, and at concentration similar to the IC50, no toxicity was evidenced. In all experiments, pentamidine isethionate was used as a reference drug. The present results reinforce the potential use of substituted hydroxyquinones and derivatives as promising antileishmanial drugs and suggest a continuing study within this class of compounds.engInstituto Oswaldo CruzAntileishmanial activity of lapachol analoguesinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleLeishmania amazonensisLeishmania braziliensisLapacholIsolapacholAntileishmanial activityNaphthoquinonesinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txttext/plain1748https://www.arca.fiocruz.br/bitstream/icict/33447/1/license.txt8a4605be74aa9ea9d79846c1fba20a33MD51ORIGINALve_Lima_Nadja_etal_INI_2004.pdfve_Lima_Nadja_etal_INI_2004.pdfapplication/pdf51749https://www.arca.fiocruz.br/bitstream/icict/33447/2/ve_Lima_Nadja_etal_INI_2004.pdff4edeba40abd3bfa0e88a83781ca7c5dMD52TEXTve_Lima_Nadja_etal_INI_2004.pdf.txtve_Lima_Nadja_etal_INI_2004.pdf.txtExtracted texttext/plain23424https://www.arca.fiocruz.br/bitstream/icict/33447/3/ve_Lima_Nadja_etal_INI_2004.pdf.txt536b65a75197ee2493c7547bc71658e9MD53icict/334472022-06-24 13:04:22.3oai:www.arca.fiocruz.br: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Repositório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352022-06-24T16:04:22Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false
dc.title.pt_BR.fl_str_mv Antileishmanial activity of lapachol analogues
title Antileishmanial activity of lapachol analogues
spellingShingle Antileishmanial activity of lapachol analogues
Lima, Nadja M. F.
Leishmania amazonensis
Leishmania braziliensis
Lapachol
Isolapachol
Antileishmanial activity
Naphthoquinones
title_short Antileishmanial activity of lapachol analogues
title_full Antileishmanial activity of lapachol analogues
title_fullStr Antileishmanial activity of lapachol analogues
title_full_unstemmed Antileishmanial activity of lapachol analogues
title_sort Antileishmanial activity of lapachol analogues
author Lima, Nadja M. F.
author_facet Lima, Nadja M. F.
Correia, Clariane S.
Leon, Leonor L.
Machado, Gérzia M. C.
Madeira, Maria de Fátima
Santana, Antônio Euzébio G.
Goulart, Marília O. F.
author_role author
author2 Correia, Clariane S.
Leon, Leonor L.
Machado, Gérzia M. C.
Madeira, Maria de Fátima
Santana, Antônio Euzébio G.
Goulart, Marília O. F.
author2_role author
author
author
author
author
author
dc.contributor.author.fl_str_mv Lima, Nadja M. F.
Correia, Clariane S.
Leon, Leonor L.
Machado, Gérzia M. C.
Madeira, Maria de Fátima
Santana, Antônio Euzébio G.
Goulart, Marília O. F.
dc.subject.en.pt_BR.fl_str_mv Leishmania amazonensis
Leishmania braziliensis
Lapachol
Isolapachol
Antileishmanial activity
Naphthoquinones
topic Leishmania amazonensis
Leishmania braziliensis
Lapachol
Isolapachol
Antileishmanial activity
Naphthoquinones
description Maria de Fátima Madeira. Fundação Oswaldo Cruz. Instituto Nacional de Infectologia Evandro Chagas. Documento produzido em parceria ou por autor vinculado à Fiocruz, mas não consta a informação no documento.
publishDate 2004
dc.date.issued.fl_str_mv 2004
dc.date.accessioned.fl_str_mv 2019-06-10T19:57:18Z
dc.date.available.fl_str_mv 2019-06-10T19:57:18Z
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 LIMA, Nadja M. F. et al. Antileishmanial activity of lapachol analogues. Memórias do Instituto Oswaldo Cruz, Rio de Janeiro, v. 99, n. 7, p. 757-761, Nov. 2004.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/33447
dc.identifier.issn.pt_BR.fl_str_mv 0074-0276
dc.identifier.doi.none.fl_str_mv 10.1590/S0074-02762004000700017
dc.identifier.eissn.none.fl_str_mv 1678-8060
identifier_str_mv LIMA, Nadja M. F. et al. Antileishmanial activity of lapachol analogues. Memórias do Instituto Oswaldo Cruz, Rio de Janeiro, v. 99, n. 7, p. 757-761, Nov. 2004.
0074-0276
10.1590/S0074-02762004000700017
1678-8060
url https://www.arca.fiocruz.br/handle/icict/33447
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
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dc.publisher.none.fl_str_mv Instituto Oswaldo Cruz
publisher.none.fl_str_mv Instituto Oswaldo Cruz
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
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