Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/31223
Title: Leishmanicidal Activity of Withanolides from Aureliana Fasciculata var. Fasciculata
Authors: 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
Affilliation: 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.
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.
Abstract: 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.
Keywords: Leishmania
Solanaceae
Withanolides
Aurelianolides
keywords: Leishmania
Vitanolídeos
Solanaceae
DeCS: Vitanolídeos
Issue Date: 2018
Publisher: MDPI
Citation: LIMA, Simone Cristina de M. et al. Leishmanicidal Activity ofWithanolides from Aureliana Fasciculata var. Fasciculata. Molecules, v.23, n.3160, 12p, 2018.
DOI: 10.3390/molecules23123160
ISSN: 1420-3049
Copyright: open access
Appears in Collections:IOC - Artigos de Periódicos

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