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In vitro Antiplasmodial Activities of Alkaloids Isolated from Roots of Worsleya procera (Lem.) Traub (Amaryllidaceae)

2019; Brazilian Chemical Society; Linguagem: Inglês

10.21577/0103-5053.20190061

1678-4790

Karla L. Gonring-Salarini, Raphael Conti, Jean Paulo de Andrade, Bárbara Juliana Pinheiro Borges, Anna Caroline Campos Aguiar, Juliana Oliveira de Souza, Camila Lima Zanini, Glaucius Oliva, Juan C. Tenório, Javier Ellena, Jaume Bastida, Rafael V. C. Guido, Warley de Souza Borges,

Psychedelics and Drug Studies

A combined phytochemical, crystallographic and biological study of Worsleya procera roots was performed.Fifteen alkaloids were identified by gas chromatography mass spectrometry (GC-MS) and seven of them were isolated.The structures of the alkaloids were elucidated by spectroscopic methods, and a detailed crystallographic study of tazettine was carried out.The isolated alkaloids and the obtained extracts were tested in vitro against Plasmodium falciparum (3D7 and K1 strains) and human hepatocarcinoma cells (HepG2) to assess their antiplasmodial and cytotoxic effects, respectively.One of the isolated alkaloid derivatives, lycorine, exhibited antiplasmodial activity against both sensitive (3D7) and resistant (K1) parasite strains in the low micromolar range (half-maximal sample inhibitory concentration (IC 50 ) values of 2.5 and 3.1 µM, respectively) and displayed a low cytotoxicity profile, with a selectivity index greater than 100.Our findings indicate that lycorine is a hit for antimalarial drug discovery.