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

Autor(es):Mostrar menos -

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]}

Afiliação do(s) autor(es)

^[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

• Tipo de documento: Artigo Científico
• Fonte: Journal of the Brazilian Chemical Society; v. 30, n. 8, p. 1624-1633, AUG 2019.
• Citações Web of Science: 0

Resumo

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)

• Processo FAPESP: 15/18192-9 - Descoberta e Desenvolvimento de Fármacos Antimaláricos: Biologia Estrutural, Química Medicinal e Parasitologia
• Beneficiário: Anna Caroline Campos Aguiar
• Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado
• Processo FAPESP: 13/07600-3 - CIBFar - Centro de Inovação em Biodiversidade e Fármacos
• Beneficiário: Glaucius Oliva
• Modalidade de apoio: Auxílio à Pesquisa - Centros de Pesquisa, Inovação e Difusão - CEPIDs
• Processo FAPESP: 17/04070-4 - Descoberta de derivados 4-quinolinonas como candidatos a composto líder para o desenvolvimento de novos antimaláricos
• Beneficiário: Juliana Oliveira de Souza
• Modalidade de apoio: Bolsas no Brasil - Iniciação Científica