Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda

Detalhes bibliográficos
Autor(a) principal: Rocha, Vinícius Pinto Costa
Data de Publicação: 2018
Outros Autores: 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
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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spelling 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:icict/33076Q0VTU8ODTyBOw4NPIEVYQ0xVU0lWQSBERSBESVJFSVRPUyBBVVRPUkFJUwoKQW8gYWNlaXRhciBvcyBURVJNT1MgZSBDT05EScOHw5VFUyBkZXN0YSBDRVNTw4NPLCBvIEFVVE9SIGUvb3UgVElUVUxBUiBkZSBkaXJlaXRvcwphdXRvcmFpcyBzb2JyZSBhIE9CUkEgZGUgcXVlIHRyYXRhIGVzdGUgZG9jdW1lbnRvOgoKKDEpIENFREUgZSBUUkFOU0ZFUkUsIHRvdGFsIGUgZ3JhdHVpdGFtZW50ZSwgw6AgRklPQ1JVWiAtIEZVTkRBw4fDg08gT1NXQUxETyBDUlVaLCBlbQpjYXLDoXRlciBwZXJtYW5lbnRlLCBpcnJldm9nw6F2ZWwgZSBOw4NPIEVYQ0xVU0lWTywgdG9kb3Mgb3MgZGlyZWl0b3MgcGF0cmltb25pYWlzIE7Dg08KQ09NRVJDSUFJUyBkZSB1dGlsaXphw6fDo28gZGEgT0JSQSBhcnTDrXN0aWNhIGUvb3UgY2llbnTDrWZpY2EgaW5kaWNhZGEgYWNpbWEsIGluY2x1c2l2ZSBvcyBkaXJlaXRvcwpkZSB2b3ogZSBpbWFnZW0gdmluY3VsYWRvcyDDoCBPQlJBLCBkdXJhbnRlIHRvZG8gbyBwcmF6byBkZSBkdXJhw6fDo28gZG9zIGRpcmVpdG9zIGF1dG9yYWlzLCBlbQpxdWFscXVlciBpZGlvbWEgZSBlbSB0b2RvcyBvcyBwYcOtc2VzOwoKKDIpIEFDRUlUQSBxdWUgYSBjZXNzw6NvIHRvdGFsIG7Do28gZXhjbHVzaXZhLCBwZXJtYW5lbnRlIGUgaXJyZXZvZ8OhdmVsIGRvcyBkaXJlaXRvcyBhdXRvcmFpcwpwYXRyaW1vbmlhaXMgbsOjbyBjb21lcmNpYWlzIGRlIHV0aWxpemHDp8OjbyBkZSBxdWUgdHJhdGEgZXN0ZSBkb2N1bWVudG8gaW5jbHVpLCBleGVtcGxpZmljYXRpdmFtZW50ZSwKb3MgZGlyZWl0b3MgZGUgZGlzcG9uaWJpbGl6YcOnw6NvIGUgY29tdW5pY2HDp8OjbyBww7pibGljYSBkYSBPQlJBLCBlbSBxdWFscXVlciBtZWlvIG91IHZlw61jdWxvLAppbmNsdXNpdmUgZW0gUmVwb3NpdMOzcmlvcyBEaWdpdGFpcywgYmVtIGNvbW8gb3MgZGlyZWl0b3MgZGUgcmVwcm9kdcOnw6NvLCBleGliacOnw6NvLCBleGVjdcOnw6NvLApkZWNsYW1hw6fDo28sIHJlY2l0YcOnw6NvLCBleHBvc2nDp8OjbywgYXJxdWl2YW1lbnRvLCBpbmNsdXPDo28gZW0gYmFuY28gZGUgZGFkb3MsIHByZXNlcnZhw6fDo28sIGRpZnVzw6NvLApkaXN0cmlidWnDp8OjbywgZGl2dWxnYcOnw6NvLCBlbXByw6lzdGltbywgdHJhZHXDp8OjbywgZHVibGFnZW0sIGxlZ2VuZGFnZW0sIGluY2x1c8OjbyBlbSBub3ZhcyBvYnJhcyBvdQpjb2xldMOibmVhcywgcmV1dGlsaXphw6fDo28sIGVkacOnw6NvLCBwcm9kdcOnw6NvIGRlIG1hdGVyaWFsIGRpZMOhdGljbyBlIGN1cnNvcyBvdSBxdWFscXVlciBmb3JtYSBkZQp1dGlsaXphw6fDo28gbsOjbyBjb21lcmNpYWw7CgooMykgUkVDT05IRUNFIHF1ZSBhIGNlc3PDo28gYXF1aSBlc3BlY2lmaWNhZGEgY29uY2VkZSDDoCBGSU9DUlVaIC0gRlVOREHDh8ODTyBPU1dBTERPCkNSVVogbyBkaXJlaXRvIGRlIGF1dG9yaXphciBxdWFscXVlciBwZXNzb2Eg4oCTIGbDrXNpY2Egb3UganVyw61kaWNhLCBww7pibGljYSBvdSBwcml2YWRhLCBuYWNpb25hbCBvdQplc3RyYW5nZWlyYSDigJMgYSBhY2Vzc2FyIGUgdXRpbGl6YXIgYW1wbGFtZW50ZSBhIE9CUkEsIHNlbSBleGNsdXNpdmlkYWRlLCBwYXJhIHF1YWlzcXVlcgpmaW5hbGlkYWRlcyBuw6NvIGNvbWVyY2lhaXM7CgooNCkgREVDTEFSQSBxdWUgYSBvYnJhIMOpIGNyaWHDp8OjbyBvcmlnaW5hbCBlIHF1ZSDDqSBvIHRpdHVsYXIgZG9zIGRpcmVpdG9zIGFxdWkgY2VkaWRvcyBlIGF1dG9yaXphZG9zLApyZXNwb25zYWJpbGl6YW5kby1zZSBpbnRlZ3JhbG1lbnRlIHBlbG8gY29udGXDumRvIGUgb3V0cm9zIGVsZW1lbnRvcyBxdWUgZmF6ZW0gcGFydGUgZGEgT0JSQSwKaW5jbHVzaXZlIG9zIGRpcmVpdG9zIGRlIHZveiBlIGltYWdlbSB2aW5jdWxhZG9zIMOgIE9CUkEsIG9icmlnYW5kby1zZSBhIGluZGVuaXphciB0ZXJjZWlyb3MgcG9yCmRhbm9zLCBiZW0gY29tbyBpbmRlbml6YXIgZSByZXNzYXJjaXIgYSBGSU9DUlVaIC0gRlVOREHDh8ODTyBPU1dBTERPIENSVVogZGUKZXZlbnR1YWlzIGRlc3Blc2FzIHF1ZSB2aWVyZW0gYSBzdXBvcnRhciwgZW0gcmF6w6NvIGRlIHF1YWxxdWVyIG9mZW5zYSBhIGRpcmVpdG9zIGF1dG9yYWlzIG91CmRpcmVpdG9zIGRlIHZveiBvdSBpbWFnZW0sIHByaW5jaXBhbG1lbnRlIG5vIHF1ZSBkaXogcmVzcGVpdG8gYSBwbMOhZ2lvIGUgdmlvbGHDp8O1ZXMgZGUgZGlyZWl0b3M7CgooNSkgQUZJUk1BIHF1ZSBjb25oZWNlIGEgUG9sw610aWNhIEluc3RpdHVjaW9uYWwgZGUgQWNlc3NvIEFiZXJ0byBkYSBGSU9DUlVaIC0gRlVOREHDh8ODTwpPU1dBTERPIENSVVogZSBhcyBkaXJldHJpemVzIHBhcmEgbyBmdW5jaW9uYW1lbnRvIGRvIHJlcG9zaXTDs3JpbyBpbnN0aXR1Y2lvbmFsIEFSQ0EuCgpBIFBvbMOtdGljYSBJbnN0aXR1Y2lvbmFsIGRlIEFjZXNzbyBBYmVydG8gZGEgRklPQ1JVWiAtIEZVTkRBw4fDg08gT1NXQUxETyBDUlVaIHJlc2VydmEKZXhjbHVzaXZhbWVudGUgYW8gQVVUT1Igb3MgZGlyZWl0b3MgbW9yYWlzIGUgb3MgdXNvcyBjb21lcmNpYWlzIHNvYnJlIGFzIG9icmFzIGRlIHN1YSBhdXRvcmlhCmUvb3UgdGl0dWxhcmlkYWRlLCBzZW5kbyBvcyB0ZXJjZWlyb3MgdXN1w6FyaW9zIHJlc3BvbnPDoXZlaXMgcGVsYSBhdHJpYnVpw6fDo28gZGUgYXV0b3JpYSBlIG1hbnV0ZW7Dp8OjbwpkYSBpbnRlZ3JpZGFkZSBkYSBPQlJBIGVtIHF1YWxxdWVyIHV0aWxpemHDp8Ojby4KCkEgUG9sw610aWNhIEluc3RpdHVjaW9uYWwgZGUgQWNlc3NvIEFiZXJ0byBkYSBGSU9DUlVaIC0gRlVOREHDh8ODTyBPU1dBTERPIENSVVoKcmVzcGVpdGEgb3MgY29udHJhdG9zIGUgYWNvcmRvcyBwcmVleGlzdGVudGVzIGRvcyBBdXRvcmVzIGNvbSB0ZXJjZWlyb3MsIGNhYmVuZG8gYW9zIEF1dG9yZXMKaW5mb3JtYXIgw6AgSW5zdGl0dWnDp8OjbyBhcyBjb25kacOnw7VlcyBlIG91dHJhcyByZXN0cmnDp8O1ZXMgaW1wb3N0YXMgcG9yIGVzdGVzIGluc3RydW1lbnRvcy4KRepositório 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
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 MDPI
publisher.none.fl_str_mv MDPI
dc.source.none.fl_str_mv reponame:Repositório Institucional da FIOCRUZ (ARCA)
instname:Fundação Oswaldo Cruz (FIOCRUZ)
instacron:FIOCRUZ
instname_str Fundação Oswaldo Cruz (FIOCRUZ)
instacron_str FIOCRUZ
institution FIOCRUZ
reponame_str Repositório Institucional da FIOCRUZ (ARCA)
collection Repositório Institucional da FIOCRUZ (ARCA)
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