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

Autor(es)

Dal Picolo, Camilla R. ^[1] ; Bezerra, Mariana P. ^[1] ; Gomes, Kaio S. ^[1] ; Passero, Luiz Felipe D. ^[2] ; Laurenti, Marcia D. ^[2] ; Martins, Euder Glendes A. ^[3] ; Sartorelli, Patricia ^[1] ; Lago, Joao Henrique G. ^[1]

Afiliação do(s) autor(es)

^[1] Univ Fed Sao Paulo, Inst Ciencias Ambientais Quim & Farmaceut, Sao Paulo - Brazil

^[2] Univ Sao Paulo, Fac Med, Dept Patol, Lab Patol Molestias Infecciosas LIM50, Sao Paulo - Brazil

^[3] Univ Sao Paulo, Inst Biociencias, Dept Bot, Sao Paulo - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Fitoterapia; v. 97, p. 28-33, SEP 2014.
• Citações Web of Science: 17

Resumo

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. (AU)

• Processo FAPESP: 11/51739-0 - Uso sustentável da biodiversidade de áreas remanescentes da Mata Atlântica do Estado de São Paulo: avaliação, isolamento e caracterização molecular de metabólitos secundários bioativos em espécies vegetais
• Beneficiário: João Henrique Ghilardi Lago
• Modalidade de apoio: Auxílio à Pesquisa - Programa BIOTA - Regular