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Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda

Rocha, Vinícius P C ; Quintino da Rocha, Cláudia ; Ferreira Queiroz, Emerson ; Marcourt, Laurence ; Vilegas, Wagner ; Grimaldi, Gabriela B ; Furrer, Pascal ; Allémann, Éric ; Wolfender, Jean-Luc ; Soares, Milena B P

Molecules (Basel, Switzerland), 2018-12, Vol.24 (1), p.1 [Periódico revisado por pares]

Switzerland: MDPI AG

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Título:
Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda
Autor: Rocha, Vinícius P C ; Quintino da Rocha, Cláudia ; Ferreira Queiroz, Emerson ; Marcourt, Laurence ; Vilegas, Wagner ; Grimaldi, Gabriela B ; Furrer, Pascal ; Allémann, Éric ; Wolfender, Jean-Luc ; Soares, Milena B P
Assuntos: Accumulation ; Amastigotes ; Amphotericin B ; Amphotericin B - therapeutic use ; Animals ; Antiprotozoal Agents - therapeutic use ; Arrabidaea ; Arrabidaea brachypoda ; Automation ; Bignoniaceae - chemistry ; Chemotherapy ; Dimers ; Drugs ; Flagella ; Flavonoids ; Flavonoids - chemistry ; Flavonoids - therapeutic use ; Golgi apparatus ; high content ; Infections ; Investigations ; Leishmania ; Leishmania - drug effects ; Leishmania - pathogenicity ; Leishmaniasis ; Macrophages ; Metabolism ; Mice ; Mice, Inbred BALB C ; Microscopy ; Microscopy, Electron ; Miltefosine ; Molecular Structure ; Morphology ; Myelin ; Parasites ; Parasitic diseases ; Promastigotes ; Toxicity ; Tropical diseases ; Vector-borne diseases ; Vesicles
É parte de: Molecules (Basel, Switzerland), 2018-12, Vol.24 (1), p.1
Notas: ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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Descrição: Leishmaniasis are diseases caused by parasites belonging to 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 . Three compounds were tested against 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 , 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 -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 .
Editor: Switzerland: MDPI AG
Idioma: Inglês

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Antileishmanial Activity of Dimeric Flavonoids Isolated from Arrabidaea brachypoda

Rocha, Vinícius P C ; Quintino da Rocha, Cláudia ; Ferreira Queiroz, Emerson ; Marcourt, Laurence ; Vilegas, Wagner ; Grimaldi, Gabriela B ; Furrer, Pascal ; Allémann, Éric ; Wolfender, Jean-Luc ; Soares, Milena B P

Switzerland: MDPI AG

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