In vitro Antiplasmodial Activities of Alkaloids Isolated from Roots of Worsleya procera (Lem.) Traub (Amaryllidaceae)
| Autor: | Juan C. Tenorio, Raphael Conti, Javier Ellena, Camila Lima Zanini, Jean Paulo de Andrade, Glaucius Oliva, Anna Caroline Campos Aguiar, Rafael Victorio Carvalho Guido, Jaume Bastida, Juliana Oliveira de Souza, Karla L. Gonring-Salarini, Warley de Souza Borges, Bárbara Juliana Pinheiro Borges |
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| Jazyk: | angličtina |
| Rok vydání: | 2019 |
| Předmět: |
Isoquinoline
biology Traditional medicine Chemistry Amaril·lidàcies Alkaloid Isoquinolina Plasmodium falciparum Amaryllidaceae General Chemistry biology.organism_classification Lycorine tazettine In vitro chemistry.chemical_compound Alkaloids lycorine Phytochemical Alcaloides heterocyclic compounds Cytotoxicity isoquinolinic alkaloids IC50 |
| Zdroj: | Dipòsit Digital de la UB Universidad de Barcelona Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual) Universidade de São Paulo (USP) instacron:USP Journal of the Brazilian Chemical Society v.30 n.8 2019 Journal of the Brazilian Chemical Society Sociedade Brasileira de Química (SBQ) instacron:SBQ Journal of the Brazilian Chemical Society, Volume: 30, Issue: 8, Pages: 1624-1633, Published: 12 AUG 2019 |
| Popis: | 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 |
| Databáze: | OpenAIRE |
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