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Title: In vitro Antiplasmodial Activities of Alkaloids Isolated from Roots of Worsleya procera (Lem.) Traub (Amaryllidaceae)
Author: Gonring-Salarini, Karla L.
Conti, Raphael
Andrade, Jean Paulo de
Borges, Bárbara Juliana P.
Aguiar, Anna Caroline C.
Souza, Juliana O.
Zanini, Camila L.
Oliva, Glaucius
Tenorio, Juan Carlos
Ellena, Javier
Bastida Armengol, Jaume
Guido, Rafael V. C.
Borges, Warley S.
Keywords: Alcaloides
Issue Date: 11-Apr-2019
Publisher: Sociedade Brasileira de Química
Abstract: 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 (IC50) 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. Keywords: isoquinolinic alkaloids; Amaryllidaceae; Plasmodium falciparum; lycorine; tazettine
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It is part of: Journal of the Brazilian Chemical Society, 2019, vol. 30, num. 8, p. 1624-1633
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ISSN: 0103-5053
Appears in Collections:Articles publicats en revistes (Biologia, Sanitat i Medi Ambient)

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