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

Author(s)

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]

Affiliation

^[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

• Document type: Journal article
• Source: CHEMISTRY & BIODIVERSITY; v. 18, n. 10 SEP 2021.
• Web of Science Citations: 0

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 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. (AU)

• FAPESP's process: 16/22488-3 - Drug repositioning for neglected diseases: identification of novel anthelmintic agents
• Grantee: Josué de Moraes
• Support Opportunities: Regular Research Grants
• FAPESP's process: 19/25289-0 - In vitro anthelmintic activity of praziquantel and mefenamic acid nanocarreated
• Grantee: Vinícius de Castro Rodrigues
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• FAPESP's process: 21/02789-7 - Search for bioactive metabolites with antiparasitic action in plant species from Atlantic Forest and Cerrado regions - a chemical, phenotypical, and metabolomic approach
• Grantee: João Henrique Ghilardi Lago
• Support Opportunities: BIOTA-FAPESP Program - Regular Research Grants
• FAPESP's process: 19/25905-2 - Preclinical evaluation for oral administration of nanostructured formulations containing drugs with anthelmintic activity
• Grantee: Ana Carolina Araujo Mengarda
• Support Opportunities: Scholarships in Brazil - Doctorate