Antileishmanial activity evaluation of adunchalcone,a new prenylated dihydrochalcone from Piper aduncum L. |
| |
| Affiliation: | 1. Instituto de Ciências Ambientais, Químicas e Farmacêuticas, Universidade Federal de São Paulo, São Paulo, Brazil;2. Laboratório de Patologia de Moléstias Infecciosas (LIM-50), Departamento de Patologia, Faculdade de Medicina, Universidade de São Paulo, São Paulo, Brazil;3. Departamento de Botânica, Instituto de Biociências, Universidade de São Paulo, São Paulo, Brazil;1. Faculdade de Farmácia, Departamento de Ciências Farmacêuticas, Universidade Federal de Juiz de Fora, R. José Lourenço Kelmer s/n, Campus Universitário, Juiz de Fora, MG, 36036-900, Brazil;2. Departamento de Química, Universidade Federal de Juiz de Fora, Juiz de Fora, MG, 36036-900, Brazil;3. Instituto de Ciências Biológicas, Universidade Federal de Juiz de Fora, Juiz de Fora, MG, 36036-900, Brazil;4. Núcleo de Pesquisa em Doenças Negligenciadas, Universidade Guarulhos, Guarulhos, SP, 07023-070, Brazil |
| |
| 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.) shawi, and L. (L.) chagasi and displayed 50% effective concentrations (EC50) of 11.03, 26.70, and 11.26 μM, 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. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
