Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda
Autor(a) principal: | |
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Data de Publicação: | 2018 |
Outros Autores: | , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da FIOCRUZ (ARCA) |
Texto Completo: | https://www.arca.fiocruz.br/handle/icict/33076 |
Resumo: | National Council for Scientific and Technological Development (CNPq), Coordination of Improvement of Higher Level Personnel (CAPES) and Foundation for Research Support of the State of Bahia (FAPESB). |
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Rocha, Vinícius Pinto CostaRocha, Cláudia Quintino daQueiroz, Emerson FerreiraMarcourt, LaurenceVilegas, WagnerGrimaldi, Gabriela BittencourtFurrer, PascalAllémann, ÉricWolfender, Jean-LucSoares, Milena Botelho Pereira2019-05-14T18:18:02Z2019-05-14T18:18:02Z2018ROCHA, Vinícius Pinto Costa et al. Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda. Molecules, v. 24, p. 1-13, 2019.1420-3049https://www.arca.fiocruz.br/handle/icict/3307610.3390/molecules24010001National Council for Scientific and Technological Development (CNPq), Coordination of Improvement of Higher Level Personnel (CAPES) and Foundation for Research Support of the State of Bahia (FAPESB).Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Laboratório de Engenharia Tecidual e e Imunofarmacologia. Salvador, BA, Brasil.Universidade Federal do Maranhão. Departamento de Química. São Luiz, MA, Brasil.University of Geneva. University of Lausanne. School of Pharmaceutical Sciences. Geneva, Switzerland.University of Geneva. University of Lausanne. School of Pharmaceutical Sciences. Geneva, Switzerland.Universidade do Estado de São Paulo. Campus Experimental do Litoral Paulista. São Paulo, SP, Brasil.Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Laboratório de Engenharia Tecidual e e Imunofarmacologia. Salvador, BA, Brasil.University of Geneva. University of Lausanne. School of Pharmaceutical Sciences. Geneva, Switzerland.University of Geneva. University of Lausanne. School of Pharmaceutical Sciences. Geneva, Switzerland.University of Geneva. University of Lausanne. School of Pharmaceutical Sciences. Geneva, Switzerland.Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Laboratório de Engenharia Tecidual e e Imunofarmacologia. Salvador, BA, Brasil.Leishmaniasis are diseases caused by parasites belonging to Leishmania genus. The treatment with pentavalent antimonials present high toxicity. Secondary line drugs, such as amphotericin B and miltefosine also have a narrow therapeutic index. Therefore, there is an urgent need to develop new drugs to treat leishmaniasis. Here, we present the in vitro anti-leishmanial activity of unusual dimeric flavonoids purified from Arrabidaea brachypoda. Three compounds were tested against Leishmana sp. Compound 2 was the most active against promastigotes. Quantifying the in vitro infected macrophages revealed that compound 2 was also the most active against intracellular amastigotes of L. amazonensis, without displaying host cell toxicity. Drug combinations presented an additive effect, suggesting the absence of interaction between amphotericin B and compound 2. Amastigotes treated with compound 2 demonstrated alterations in the Golgi and accumulation of vesicles inside the flagellar pocket. Compound 2-treated amastigotes presented a high accumulation of cytoplasmic vesicles and a myelin-like structure. When administered in L. amazonensis-infected mice, neither the oral nor the topical treatments were effective against the parasite. Based on the high in vitro activity, dimeric flavonoids can be used as a lead structure for the development of new molecules that could be useful for structure-active studies against Leishmania.engMDPILeishmaniaFlavonóidesAlto teorBrachypoda de ArrabidaeaLeishmaniaFlavonoidsHigh contentArrabidaea brachypodaAntileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypodainfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-82991https://www.arca.fiocruz.br/bitstream/icict/33076/1/license.txt5a560609d32a3863062d77ff32785d58MD51ORIGINALRocha V.P. Antileishmanial Activity 2019.pdfRocha V.P. Antileishmanial Activity 2019.pdfapplication/pdf3368752https://www.arca.fiocruz.br/bitstream/icict/33076/2/Rocha%20V.P.%20Antileishmanial%20Activity%202019.pdfd4e6f8663f2397361517ad7060201dadMD52TEXTRocha V.P. Antileishmanial Activity 2019.pdf.txtRocha V.P. Antileishmanial Activity 2019.pdf.txtExtracted texttext/plain59534https://www.arca.fiocruz.br/bitstream/icict/33076/3/Rocha%20V.P.%20Antileishmanial%20Activity%202019.pdf.txtad38ee2cba0ac8662cf89149da52808aMD53icict/330762023-03-15 14:34:22.096oai:www.arca.fiocruz.br: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ório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352023-03-15T17:34:22Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false |
dc.title.pt_BR.fl_str_mv |
Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda |
title |
Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda |
spellingShingle |
Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda Rocha, Vinícius Pinto Costa Leishmania Flavonóides Alto teor Brachypoda de Arrabidaea Leishmania Flavonoids High content Arrabidaea brachypoda |
title_short |
Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda |
title_full |
Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda |
title_fullStr |
Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda |
title_full_unstemmed |
Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda |
title_sort |
Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda |
author |
Rocha, Vinícius Pinto Costa |
author_facet |
Rocha, Vinícius Pinto Costa Rocha, Cláudia Quintino da Queiroz, Emerson Ferreira Marcourt, Laurence Vilegas, Wagner Grimaldi, Gabriela Bittencourt Furrer, Pascal Allémann, Éric Wolfender, Jean-Luc Soares, Milena Botelho Pereira |
author_role |
author |
author2 |
Rocha, Cláudia Quintino da Queiroz, Emerson Ferreira Marcourt, Laurence Vilegas, Wagner Grimaldi, Gabriela Bittencourt Furrer, Pascal Allémann, Éric Wolfender, Jean-Luc Soares, Milena Botelho Pereira |
author2_role |
author author author author author author author author author |
dc.contributor.author.fl_str_mv |
Rocha, Vinícius Pinto Costa Rocha, Cláudia Quintino da Queiroz, Emerson Ferreira Marcourt, Laurence Vilegas, Wagner Grimaldi, Gabriela Bittencourt Furrer, Pascal Allémann, Éric Wolfender, Jean-Luc Soares, Milena Botelho Pereira |
dc.subject.other.pt_BR.fl_str_mv |
Leishmania Flavonóides Alto teor Brachypoda de Arrabidaea |
topic |
Leishmania Flavonóides Alto teor Brachypoda de Arrabidaea Leishmania Flavonoids High content Arrabidaea brachypoda |
dc.subject.en.pt_BR.fl_str_mv |
Leishmania Flavonoids High content Arrabidaea brachypoda |
description |
National Council for Scientific and Technological Development (CNPq), Coordination of Improvement of Higher Level Personnel (CAPES) and Foundation for Research Support of the State of Bahia (FAPESB). |
publishDate |
2018 |
dc.date.issued.fl_str_mv |
2018 |
dc.date.accessioned.fl_str_mv |
2019-05-14T18:18:02Z |
dc.date.available.fl_str_mv |
2019-05-14T18:18:02Z |
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 |
ROCHA, Vinícius Pinto Costa et al. Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda. Molecules, v. 24, p. 1-13, 2019. |
dc.identifier.uri.fl_str_mv |
https://www.arca.fiocruz.br/handle/icict/33076 |
dc.identifier.issn.pt_BR.fl_str_mv |
1420-3049 |
dc.identifier.doi.none.fl_str_mv |
10.3390/molecules24010001 |
identifier_str_mv |
ROCHA, Vinícius Pinto Costa et al. Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda. Molecules, v. 24, p. 1-13, 2019. 1420-3049 10.3390/molecules24010001 |
url |
https://www.arca.fiocruz.br/handle/icict/33076 |
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eng |
language |
eng |
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info:eu-repo/semantics/openAccess |
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openAccess |
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MDPI |
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MDPI |
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