Evaluation of Gibbilimbol B, Isolated from Piper malacophyllum (Piperaceae), as an Antischistosomal Agent

被引：6
作者：
Carnauba, Paulo U. [1 ]
Mengarda, Ana C. [1 ]
Rodrigues, Vinicius C. [1 ]
Morais, Thiago R. [1 ]
de Oliveira, Alberto [2 ]
Lago, Joao Henrique G. [3 ]
de Moraes, Josue [1 ]
机构：
[1] Univ Guarulhos, Nucleo Pesquisa Doencas Negligenciadas, Praca Tereza Cristina 88, BR-07023070 Guarulhos, SP, Brazil
[2] Univ Fed Uberlandia, Inst Quim, Av Joao Naves de Avila 2121, BR-38408100 Uberlandia, MG, Brazil
[3] Univ Fed ABC, Ctr Ciencias Nat & Humanas, Ave Estados 5001, BR-09210580 Santo Andre, SP, Brazil
来源：
CHEMISTRY & BIODIVERSITY | 2021年 / 18卷 / 10期
基金：
巴西圣保罗研究基金会;
关键词：
schistosomiasis; neglected tropical diseases; natural product; schistosomicidal activity; antischistosomal compound; ANTIPARASITIC ACTIVITY; ANTHELMINTIC ACTIVITY; SCHISTOSOMA; ANTIBACTERIAL; ANALOGS; DRUGS;
D O I：
10.1002/cbdv.202100503
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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 mu M, 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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页数：8
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