Antileishmanial activity evaluation of adunchalcone, a new prenylated dihydrochalcone from Piper aduncum L.

Antileishmanial activity evaluation of adunchalcone, a new prenylated dihydrochalcone from Piper aduncum L.

Author Dal Picolo, Camilla R. Autor UNIFESP Google Scholar
Bezerra, Mariana P. Autor UNIFESP Google Scholar
Gomes, Kaio S. Autor UNIFESP Google Scholar
Passero, Luiz Felipe D. Google Scholar
Laurenti, Marcia D. Google Scholar
Martins, Euder Glendes A. Google Scholar
Sartorelli, Patricia Autor UNIFESP Google Scholar
Lago, Joao Henrique G. Autor UNIFESP Google Scholar
Institution Universidade Federal de São Paulo (UNIFESP)
Universidade de São Paulo (USP)
Abstract Bioactivity-guided fractionation of EtOH extract from the leaves of Piper aduncum L. (Piperaceae) afforded a new dihydrochalcone, named adunchalcone. Its structure was elucidated on the basis of their spectroscopic data, primarily NMR and MS. Adunchalcone was evaluated against promastigote forms of Leishmania (L.) amazonensis, L. (V.) braziliensis, L. (V.) shawl, and L. (L.) chagasi and displayed 50% effective concentrations (EC50) of 11.03, 26.70, and 11.26 mu M, as well as selective indexes of 4.86, 2.01, 4.76 and 0.50, respectively. This compound was also tested against intracellular forms of L. (L.) amazonensis, displaying weak activity, in comparison to reference drug amphotericin B. However, despite reduced effect of adunchalcone against amastigotes of L. (L.) amazonensis, this work opens the perspective to use this particular molecule as a scaffold for the design of novel and selective drug candidates for neglected diseases, mainly leishmaniasis. (c) 2014 Elsevier B.V. All rights reserved.
Keywords Piper aduncum
Piperaceae
Antileishmanial
Dihydrochalcone
Adunchalcone
Language English
Sponsor Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
Grant number FAPESP: FAPESP - 2011/51739-0
CNPq: CNPq - 470853/2012-3
Date 2014-09-01
Published in Fitoterapia. Amsterdam: Elsevier B.V., v. 97, p. 28-33, 2014.
ISSN 0367-326X (Sherpa/Romeo, impact factor)
Publisher Elsevier B.V.
Extent 28-33
Origin http://dx.doi.org/10.1016/j.fitote.2014.05.009
Access rights Closed access
Type Article
Web of Science ID WOS:000341346400004
URI http://repositorio.unifesp.br/handle/11600/38164

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