In Vitro Cytotoxic and Leishmanicidal Activity of Isolated and Semisynthetic ent -Pimaranes from Aldama arenaria

Autor(es)

Santos de Oliveira, Adriana da Silva ; Conrado, Gabrielly Galdino ; Grazzia, Nathalia ; Miguel, Danilo Ciccone ; Franchi Junior, Gilberto Carlos ; Garcia, Vera Lucia

• Tipo de documento: Artigo Científico
• Fonte: Planta Medica; v. 88, n. 13, p. 12-pg., 2022-02-10.

Resumo

Two pimaranes ent -pimara-8(14),15-dien-19-oic acid ( 1 ) and ent -8(14),15-pimaradien-3 beta -ol ( 2 ), isolated from Aldama arenaria , and six semi-synthetic derivatives methyl ester of the ent -pimara-8(14),15-dien-19-oic acid ( 3 ), ent -pimara-8(14),15-dien-19-ol ( 4 ), acetate of ent -pimara-8(14),15-dien-19-ol ( 5 ), ent -pimara-8(14),15-dien-19-ol succinic acid ( 6 ), acetate of ent -8(14),15-pimaradien-3 beta -ol ( 7 ), ent -8(14),15-pimaradien-3 beta -ol succinic acid ( 8 ) were evaluated in vitro for their cytotoxic activities to childhood leukemia cell lines and leishmanicidal activity against the parasite Leishmania amazonensis. Among these compounds, 1 to 6 presented moderate cytotoxic activity, with compound 4 being the most active (GI (50) of 2.6 mu M for the HL60 line) and the derivatives 7 and 8 being inactive. Against the parasite Leishmania amazonensis , the most promising derivative was the acetate of ent -pimara-8(14),15-dien-19-ol ( 5 ), with EC (50) of 20.1 mu M, selectivity index of 14.5, and significant reduction in the parasite load. Pimarane analogues 1 , ent -pimara-8(14),15-dien-19-oic acid, and 2 , ent -8(14),15-pimaradien-3 beta -ol, presented different activities, corroborating the application of such molecules as prototypes for the design of other derivatives that have greater cytotoxic or leishmanicidal potential. (AU)

• Processo FAPESP: 10/51454-3 - Estudos morfoanatômicos, metabolômicos e moleculares como subsídios à sistemática de espécies de Asteraceae e acesso ao seu potencial farmacológico
• Beneficiário: Beatriz Appezzato da Glória
• Modalidade de apoio: Auxílio à Pesquisa - Temático