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

Author(s):Show less -

Gonring-Salarini, Karla L. ^[1] ; Conti, Raphael ^[2] ; de Andrade, Jean Paulo ^[1] ; Borges, Barbara Juliana P. ^[1] ; Aguiar, Anna Caroline C. ^[3] ; de Souza, Juliana O. ^[3] ; Zanini, Camila L. ^[3] ; Oliva, Glaucius ^[3] ; Tenorio, Juan Carlos ^[4] ; Ellena, Javier ^[4] ; Bastida, Jaume ^[5] ; Guido, Rafael V. C. ^[3] ; Borges, Warley de S. ^{[1, 2]}

Affiliation

^[1] Univ Fed Espirito Santo, Dept Ciencias Farmaceut, Av Marechal Campos 1468, BR-29043900 Vitoria, ES - Brazil

^[2] Univ Fed Espirito Santo, Dept Quim, Av Fernando Ferrari 514, BR-29043900 Vitoria, ES - Brazil

^[3] Univ Sao Paulo, Inst Fis Sao Carlos, Av Joao Dagnone 1100, BR-13563120 Sao Carlos, SP - Brazil

^[4] Univ Sao Paulo, Inst Fis Sao Carlos, Lab Multiusuario Cristalog Estrutural, Av Trabalhador Sao Carlense 400, BR-13560570 Sao Carlos, SP - Brazil

^[5] Univ Barcelona, Fac Farm, Dept Biol Sanitat & Medi Ambient, Av Joan XXIII 27-31, E-08028 Barcelona - Spain

• Document type: Journal article
• Source: Journal of the Brazilian Chemical Society; v. 30, n. 8, p. 1624-1633, AUG 2019.
• Web of Science Citations: 0

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. (AU)

• FAPESP's process: 15/18192-9 - Discovery and development of Antimalarial Drugs: Structural Biology, Medicinal Chemistry and Parasitology
• Grantee: Anna Caroline Campos Aguiar
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery
• Grantee: Glaucius Oliva
• Support Opportunities: Research Grants - Research, Innovation and Dissemination Centers - RIDC
• FAPESP's process: 17/04070-4 - Discovery of 4-quinolinones derivatives as lead compound candidates for the development of new antimalarials
• Grantee: Juliana Oliveira de Souza
• Support Opportunities: Scholarships in Brazil - Scientific Initiation