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Molecules 2019, 24(1), 1; https://doi.org/10.3390/molecules24010001

Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda

1
Laboratório de Engenharia Tecidual e Imunofarmacologia, Instituto Gonçalo Moniz, Fundação Oswaldo Cruz (Fiocruz), Avenida Waldemar Falcão, 121, Candeal–Salvador-BA 40296-710, Brazil
2
Departamento de Química, Universidade Federal do Maranhão, São Luiz 65080-805, MA, Brazil
3
School of Pharmaceutical Sciences, EPGL, University of Geneva, University of Lausanne, CMU, 1, Rue Michel Servet, 1211 Geneva, Switzerland
4
UNESP-Campus Experimental do Litoral Paulista, Praça Infante Dom Henrique s/n°, Parque Bitaru, São Vicente–SP 11330-900, Brazil
*
Author to whom correspondence should be addressed.
Academic Editor: Thomas J. Schmidt
Received: 20 November 2018 / Revised: 10 December 2018 / Accepted: 19 December 2018 / Published: 20 December 2018
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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. View Full-Text
Keywords: Leishmania; flavonoids; high content; Arrabidaea brachypoda Leishmania; flavonoids; high content; Arrabidaea brachypoda
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Rocha, V.P.C.; Quintino da Rocha, C.; Ferreira Queiroz, E.; Marcourt, L.; Vilegas, W.; Grimaldi, G.B.; Furrer, P.; Allémann, É.; Wolfender, J.-L.; Soares, M.B.P. Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda. Molecules 2019, 24, 1.

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