Cardamonin, a schistosomicidal chalcone from Piper aduncum L. (Piperaceae) that inhibits Schistosoma mansoni ATP diphosphohydrolase

Phytomedicine : International Journal of Phytotherapy and Phytopharmacology
Clarissa C B de CastroAdemar A Da Silva Filho

Abstract

Schistosomiasis is one of the world's major public health problems, and praziquantel (PZQ) is the only available drug to treat this neglected disease with an urgent demand for new drugs. Recent studies indicated that extracts from Piper aduncum L. (Piperaceae) are active against adult worms of Schistosoma mansoni, the major etiological agent of human schistosomiasis. We investigated the in vitro schistosomicidal activity of cardamonin, a chalcone isolated from the crude extract of P. aduncum. Also, this present work describes, for the first time, the S. mansoni ATP diphosphohydrolase inhibitory activity of cardamonin, as well as, its molecular docking with S. mansoni ATPDase1, in order to investigate its mode of inhibition. In vitro schistosomicidal assays and confocal laser scanning microscopy were used to evaluate the effects of cardamonin on adult schistosomes. Cell viability was measured by MTT assay, and the S. mansoni ATPase activity was determined spectrophotometrically. Identification of the cardamonin binding site and its interactions on S. mansoni ATPDase1 were made by molecular docking experiments. A bioguided fractionation of the crude extract of P. aduncum was carried out, leading to identification of cardamonin as...Continue Reading

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Citations

Sep 8, 2016·Chemistry & Biodiversity·Yamilet GutiérrezWilliam N Setzer
Jan 24, 2017·Phytotherapy Research : PTR·Jefferson A RochaJosé R S A Leite
Oct 3, 2018·Chemistry & Biodiversity·Vinícius R D PereiraAdemar A Da Silva Filho
Dec 19, 2018·Antimicrobial Agents and Chemotherapy·Rafael A GuerraJosué de Moraes
Jun 22, 2019·Current Topics in Medicinal Chemistry·Josué de MoraesDaniel B Roquini
Dec 17, 2016·Evidence-based Complementary and Alternative Medicine : ECAM·Luísa Maria Silveira de AlmeidaAdemar A Da Silva Filho
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Oct 6, 2021·Chemistry & Biodiversity·Lara Soares Aleixo de CarvalhoAdemar Alves Da Silva Filho

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