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

Autor(es)

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]

Afiliação do(s) autor(es)

^[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

• Tipo de documento: Artigo Científico
• Fonte: CHEMISTRY & BIODIVERSITY; v. 18, n. 10 SEP 2021.
• Citações Web of Science: 0

Resumo

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)

• Processo FAPESP: 16/22488-3 - Reposicionamento de fármacos para doenças negligenciadas: identificação de novos agentes anti-helmínticos
• Beneficiário: Josué de Moraes
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 19/25289-0 - Atividade anti-helmíntica in vitro do praziquantel e ácido mefenâmico nanocarreados
• Beneficiário: Vinícius de Castro Rodrigues
• Modalidade de apoio: Bolsas no Brasil - Iniciação Científica
• Processo FAPESP: 21/02789-7 - Busca de metabólitos bioativos com ação antiparasitária em espécies vegetais de regiões de Mata Atlântica e Cerrado - uma abordagem química, fenotípica e metabolômica
• Beneficiário: João Henrique Ghilardi Lago
• Modalidade de apoio: Auxílio à Pesquisa - Programa BIOTA - Regular
• Processo FAPESP: 19/25905-2 - Avaliação pré-clínica para administração oral de formulações nanoestruturadas contendo fármacos com atividade anti-helmíntica
• Beneficiário: Ana Carolina Araujo Mengarda
• Modalidade de apoio: Bolsas no Brasil - Doutorado