Evaluation of Gibbilimbol B,Isolated from Piper malacophyllum (Piperaceae), as an Antischistosomal Agent |
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| Authors: | Paulo U Carnaúba Ana C Mengarda Vinícius C Rodrigues Thiago R Morais Alberto de Oliveira João Henrique G Lago Josué de Moraes |
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| Institution: | 1. Núcleo de Pesquisa em Doenças Negligenciadas, Universidade Guarulhos, Praça Tereza Cristina, 88, Guarulhos, SP, 07023-070 Brazil;2. Instituto de Química, Universidade Federal de Uberlândia, Av. João Naves de Ávila, 2121, Uberlândia, MG, 38408-100 Brazil;3. Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, Avenida dos Estados, 5001, Santo André, SP, 09210-580 Brazil |
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| Abstract: | Infections caused by parasitic worms impose a considerable worldwide health burden. One of the most impactful is schistosomiasis, a disease caused by blood-dwelling of the genus Schistosoma that affects more than 230 million people worldwide. Since praziquantel has also been extensively used to treat schistosomiasis and other parasitic flatworm infections, there is an urgent need to identify novel anthelmintic compounds, mainly from natural sources. In this study, the hexane extract from roots of Piper malacophyllum (Piperaceae) showed to be mainly composed for gibbilimbol B by HPLC/ESI-HRMS. Based on this result, this compound was isolated by chromatographic steps and its structure was confirmed by NMR. In vitro bioassays showed that gibbilimbol B was more active than praziquantel against larval stage of S. mansoni, with effective concentrations of 50 % (EC50) and 90 % (EC90) values of 2.6 and 3.4 μM, respectively. Importantly, gibbilimbol B showed no cytotoxicity to mammalian cells at a concentration 190 times greater than the antiparasitic effect, giving support for the anthelmintic potential of gibbilimbol B as lead compound for novel antischistosomal agents. |
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| Keywords: | schistosomiasis neglected tropical diseases natural product schistosomicidal activity antischistosomal compound |
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