Chemical Prospection of Qualea grandiflora Mart. Fruit and Stem Extracts and Their in vitro and in vivo Antiplasmodial Activity

Autor(es):Mostrar menos -

Goncalves Neto, Geraldo S. ^[1] ; da Costa, Romario P. ^[2] ; Zanini, Camila L. ^[3] ; Aguiar, Anna Caroline C. ^[3] ; de Souza, Juliana O. ^[3] ; de Souza, Guilherme E. ^[3] ; Severino, Richele P. ^{[1, 4]} ; Cass, Quezia B. ^[2] ; Cruz, Fabio C. ^[5] ; Oliva, Glaucius ^[3] ; Guido, Rafael V. C. ^[3] ; de Sousa, Lorena R. F. ^{[1, 4]}

Afiliação do(s) autor(es)

^[1] Univ Fed Goias, Unidade Acad Especial Quim, BR-75704020 Catalao, Go - Brazil

^[2] Univ Fed Sao Carlos, Dept Quim, BR-13565905 Sao Carlos, SP - Brazil

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

^[4] Cruz, Fabio C., Univ Fed Sao Paulo, Dept Farmacol, BR-04023062 Sao Paulo, SP, Brazil.Goncalves Neto, Geraldo S., Univ Fed Goias, Unidade Acad Especial Quim, BR-75704020 Catalao, Go - Brazil

^[5] Univ Fed Sao Paulo, Dept Farmacol, BR-04023062 Sao Paulo, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Journal of the Brazilian Chemical Society; v. 31, n. 7, p. 1475-1484, JUL 2020.
• Citações Web of Science: 0

Resumo

Qualea grandiflora Mart. (“pau-terra”) is a medicinal plant symbolic from Cerrado biome. Qualea species reportedly have antiparasitic properties, but their active compounds have yet to be identified. In this study, we investigated the antiplasmodial activity of Q. grandiflora fruit and stem extracts against Plasmodium falciparum. The polar extracts of both fruits and stems showed promising in vitro antiplasmodial activity against sensitive and resistant P. falciparum strains (half-maximal inhibitory concentration (IC50) = 1.2 and 4.2 ng mL-1, respectively), low cytotoxicity against human hepatic cells (IC50HepG2 ≥ 400 ng mL-1), and a noteworthy selectivity index (SI ≥ 322 and ≥ 96, respectively). The fruit ethanolic extract revealed significant oral efficacy at 100 mg kg-1 in a mouse model of P. berghei malaria (100% reduction in parasitemia on day 5 post-infection). To investigate the chemical composition of the extracts, we developed a method involving liquid chromatography-high resolution quadrupole-time of flight mass spectrometer. The chemical profiling of active extracts indicated 32 compounds, including gallotannins, ellagic acid derivatives and flavonoids. The common component in the active polar extracts was found to be ellagic acid (EA), which may contribute favorably to the in vitro and in vivo inhibitory activity observed in this study. (AU)

• Processo FAPESP: 13/01710-1 - Ligantes enzimáticos: novos modelos de triagem
• Beneficiário: Quezia Bezerra Cass
• Modalidade de apoio: Auxílio à Pesquisa - Temático
• 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: 14/50244-6 - UHPLC acoplado a espectrômetro de massa do tipo híbrido com analisador quadrupolar e time of flight
• Beneficiário: Quezia Bezerra Cass
• Modalidade de apoio: Auxílio à Pesquisa - Programa Equipamentos Multiusuários