RESUMO
A series of lupeol derivatives 2, 2a-2f, 2a-2h, 3a-3e, and 4a-4b were designed, synthesised and evaluated for their α-glucosidase inhibitory and cytotoxic activities. Among synthetic derivatives, lupeol analogues 2b and 2e containing a benzylidene chain exhibited the best activity against α-glucosidase and superior to the positive agent with the IC50 values of 29.4 ± 1.33 and 20.1 ± 0.91 µM, respectively. Lupeol analogues 2d and 3a showed weak cytotoxicity against K562 cell line with the IC50 values of 76.6 ± 2.40 and 94.4 ± 1.51 µM, respectively.
Assuntos
Antineoplásicos , alfa-Glucosidases , Antineoplásicos/farmacologia , Estrutura Molecular , Triterpenos Pentacíclicos/farmacologia , Relação Estrutura-Atividade , alfa-Glucosidases/metabolismoRESUMO
Trichostemonoate (1), a new tirucallane, together with four known compounds, 11α,20-dihydroxydammar-24-ene-3-one (2), sapelin E acetate (3), grandifolinolenenone (4) and α-mangostin (5), were isolated from the stem bark of Walsura trichostemon. The structural assignment of the new compound was based on spectroscopic methods. All isolated compounds were evaluated for their cytotoxicity against five cancer cell lines.