Author | Rocha, Vinícius Pinto Costa | |
Author | Rocha, Cláudia Quintino da | |
Author | Queiroz, Emerson Ferreira | |
Author | Marcourt, Laurence | |
Author | Vilegas, Wagner | |
Author | Grimaldi, Gabriela Bittencourt | |
Author | Furrer, Pascal | |
Author | Allémann, Éric | |
Author | Wolfender, Jean-Luc | |
Author | Soares, Milena Botelho Pereira | |
Access date | 2019-05-14T18:18:02Z | |
Available date | 2019-05-14T18:18:02Z | |
Document date | 2018 | |
Citation | ROCHA, Vinícius Pinto Costa et al. Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda. Molecules, v. 24, p. 1-13, 2019. | pt_BR |
ISSN | 1420-3049 | pt_BR |
URI | https://www.arca.fiocruz.br/handle/icict/33076 | |
Sponsorship | 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). | pt_BR |
Language | eng | pt_BR |
Publisher | MDPI | pt_BR |
Rights | open access | pt_BR |
Subject in Portuguese | Leishmania | pt_BR |
Subject in Portuguese | Flavonóides | pt_BR |
Subject in Portuguese | Alto teor | pt_BR |
Subject in Portuguese | Brachypoda de Arrabidaea | pt_BR |
Title | Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda | pt_BR |
Type | Article | pt_BR |
DOI | 10.3390/molecules24010001 | |
Abstract | 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. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Laboratório de Engenharia Tecidual e e Imunofarmacologia. Salvador, BA, Brasil. | pt_BR |
Affilliation | Universidade Federal do Maranhão. Departamento de Química. São Luiz, MA, Brasil. | pt_BR |
Affilliation | University of Geneva. University of Lausanne. School of Pharmaceutical Sciences. Geneva, Switzerland. | pt_BR |
Affilliation | University of Geneva. University of Lausanne. School of Pharmaceutical Sciences. Geneva, Switzerland. | pt_BR |
Affilliation | Universidade do Estado de São Paulo. Campus Experimental do Litoral Paulista. São Paulo, SP, Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Laboratório de Engenharia Tecidual e e Imunofarmacologia. Salvador, BA, Brasil. | pt_BR |
Affilliation | University of Geneva. University of Lausanne. School of Pharmaceutical Sciences. Geneva, Switzerland. | pt_BR |
Affilliation | University of Geneva. University of Lausanne. School of Pharmaceutical Sciences. Geneva, Switzerland. | pt_BR |
Affilliation | University of Geneva. University of Lausanne. School of Pharmaceutical Sciences. Geneva, Switzerland. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Laboratório de Engenharia Tecidual e e Imunofarmacologia. Salvador, BA, Brasil. | pt_BR |
Subject | Leishmania | pt_BR |
Subject | Flavonoids | pt_BR |
Subject | High content | pt_BR |
Subject | Arrabidaea brachypoda | pt_BR |