Leishmanicidal Activity of Withanolides from Aureliana Fasciculata var. Fasciculata

Detalhes bibliográficos
Autor(a) principal: Lima, Simone Cristina de M.
Data de Publicação: 2018
Outros Autores: Pacheco, Juliana da Silva, Marques, André M., Veltri, Eduardo Raul Pereira, Lafetá, Rita de Cássia Almeida, Figueiredo, Maria Raquel, Kaplan, Maria Auxiliadora Coelho, Santos, Eduardo Caio Torres
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/31223
Resumo: Universidade Federal do Rio de Janeiro. Instituto de Pesquisas de Produtos Naturais. Rio de Janeiro, RJ, Brasil.
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spelling Lima, Simone Cristina de M.Pacheco, Juliana da SilvaMarques, André M.Veltri, Eduardo Raul PereiraLafetá, Rita de Cássia AlmeidaFigueiredo, Maria RaquelKaplan, Maria Auxiliadora CoelhoSantos, Eduardo Caio Torres2019-01-22T14:32:24Z2019-01-22T14:32:24Z2018LIMA, Simone Cristina de M. et al. Leishmanicidal Activity ofWithanolides from Aureliana Fasciculata var. Fasciculata. Molecules, v.23, n.3160, 12p, 2018.1420-3049https://www.arca.fiocruz.br/handle/icict/3122310.3390/molecules23123160engMDPILeishmaniaVitanolídeosSolanaceaeLeishmaniaSolanaceaeWithanolidesAurelianolidesVitanolídeosLeishmanicidal Activity of Withanolides from Aureliana Fasciculata var. Fasciculatainfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleUniversidade Federal do Rio de Janeiro. Instituto de Pesquisas de Produtos Naturais. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Tripanossomatídeos. Rio de Janeiro, RJ. Brasil.Fundação Oswaldo Cruz. Farmanguinhos. Departamento de Produtos Naturais. Rio de Janeiro, RJ. Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Tripanossomatídeos. Rio de Janeiro, RJ. Brasil.Faculdade de Educação Tecnológica do Rio de Janeiro. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Farmanguinhos. Departamento de Produtos Naturais. Rio de Janeiro, RJ. Brasil.Universidade Federal do Rio de Janeiro. Instituto de Pesquisas de Produtos Naturais. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Tripanossomatídeos. Rio de Janeiro, RJ. Brasil.Leishmaniasis is the generic denomination to the neglected diseases caused by more than 20 species of protozoa belonging to the genus Leishmania. The toxic and parenteral-delivered pentavalent antimonials remain to be the first-line treatment. However, all the current used drugs have restrictions. The species Aureliana fasciculata (Vell.) Sendtner var. fasciculata is a native Brazilian species parsimoniously studied on a chemical point of view. In this study, the antileishmanial activity of A. fasciculata was evaluated. Among the evaluated samples of the leaves, the dichloromethane partition (AFfDi) showed the more pronounced activity, with IC50 1.85 µg/ml against promastigotes of L. amazonensis. From AFfDi, two active withanolides were isolated, the Aurelianolides A and B, with IC50 7.61 μM and 7.94 μM, respectively. The withanolides also proved to be active against the clinically important form, the intracellular amastigote, with IC50 2.25 μM and 6.43 μM for Aurelianolides A and B, respectively. Furthermore, withanolides showed results for in silico parameters of absorption, distribution, metabolism, excretion, and toxicity (ADMET) similar to miltefosine, the reference drug, and were predicted as good oral drugs, with the advantage of not being hepatotoxic. These results suggest that these compounds can be useful as scaffolds for planning drug design.info: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/31223/1/license.txt5a560609d32a3863062d77ff32785d58MD51ORIGINALeduardoraul_veltri_etal_IOC_2018.pdfeduardoraul_veltri_etal_IOC_2018.pdfapplication/pdf754382https://www.arca.fiocruz.br/bitstream/icict/31223/2/eduardoraul_veltri_etal_IOC_2018.pdf4984e3bdebe219047c9a9d1b46f8238dMD52TEXTeduardoraul_veltri_etal_IOC_2018.pdf.txteduardoraul_veltri_etal_IOC_2018.pdf.txtExtracted texttext/plain47417https://www.arca.fiocruz.br/bitstream/icict/31223/3/eduardoraul_veltri_etal_IOC_2018.pdf.txt828544af0b3a737791888c6967373024MD53icict/312232019-01-23 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dc.title.pt_BR.fl_str_mv Leishmanicidal Activity of Withanolides from Aureliana Fasciculata var. Fasciculata
title Leishmanicidal Activity of Withanolides from Aureliana Fasciculata var. Fasciculata
spellingShingle Leishmanicidal Activity of Withanolides from Aureliana Fasciculata var. Fasciculata
Lima, Simone Cristina de M.
Leishmania
Vitanolídeos
Solanaceae
Leishmania
Solanaceae
Withanolides
Aurelianolides
Vitanolídeos
title_short Leishmanicidal Activity of Withanolides from Aureliana Fasciculata var. Fasciculata
title_full Leishmanicidal Activity of Withanolides from Aureliana Fasciculata var. Fasciculata
title_fullStr Leishmanicidal Activity of Withanolides from Aureliana Fasciculata var. Fasciculata
title_full_unstemmed Leishmanicidal Activity of Withanolides from Aureliana Fasciculata var. Fasciculata
title_sort Leishmanicidal Activity of Withanolides from Aureliana Fasciculata var. Fasciculata
author Lima, Simone Cristina de M.
author_facet Lima, Simone Cristina de M.
Pacheco, Juliana da Silva
Marques, André M.
Veltri, Eduardo Raul Pereira
Lafetá, Rita de Cássia Almeida
Figueiredo, Maria Raquel
Kaplan, Maria Auxiliadora Coelho
Santos, Eduardo Caio Torres
author_role author
author2 Pacheco, Juliana da Silva
Marques, André M.
Veltri, Eduardo Raul Pereira
Lafetá, Rita de Cássia Almeida
Figueiredo, Maria Raquel
Kaplan, Maria Auxiliadora Coelho
Santos, Eduardo Caio Torres
author2_role author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Lima, Simone Cristina de M.
Pacheco, Juliana da Silva
Marques, André M.
Veltri, Eduardo Raul Pereira
Lafetá, Rita de Cássia Almeida
Figueiredo, Maria Raquel
Kaplan, Maria Auxiliadora Coelho
Santos, Eduardo Caio Torres
dc.subject.other.pt_BR.fl_str_mv Leishmania
Vitanolídeos
Solanaceae
topic Leishmania
Vitanolídeos
Solanaceae
Leishmania
Solanaceae
Withanolides
Aurelianolides
Vitanolídeos
dc.subject.en.pt_BR.fl_str_mv Leishmania
Solanaceae
Withanolides
Aurelianolides
dc.subject.decs.pt_BR.fl_str_mv Vitanolídeos
description Universidade Federal do Rio de Janeiro. Instituto de Pesquisas de Produtos Naturais. Rio de Janeiro, RJ, Brasil.
publishDate 2018
dc.date.issued.fl_str_mv 2018
dc.date.accessioned.fl_str_mv 2019-01-22T14:32:24Z
dc.date.available.fl_str_mv 2019-01-22T14:32:24Z
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, Simone Cristina de M. et al. Leishmanicidal Activity ofWithanolides from Aureliana Fasciculata var. Fasciculata. Molecules, v.23, n.3160, 12p, 2018.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/31223
dc.identifier.issn.pt_BR.fl_str_mv 1420-3049
dc.identifier.doi.none.fl_str_mv 10.3390/molecules23123160
identifier_str_mv LIMA, Simone Cristina de M. et al. Leishmanicidal Activity ofWithanolides from Aureliana Fasciculata var. Fasciculata. Molecules, v.23, n.3160, 12p, 2018.
1420-3049
10.3390/molecules23123160
url https://www.arca.fiocruz.br/handle/icict/31223
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)
bitstream.url.fl_str_mv https://www.arca.fiocruz.br/bitstream/icict/31223/1/license.txt
https://www.arca.fiocruz.br/bitstream/icict/31223/2/eduardoraul_veltri_etal_IOC_2018.pdf
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