Design and synthesis of new lupeol derivatives and their α-glucosidase inhibitory and cytotoxic activities.

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.

Citation

Hoang-Vinh-Truong Phan, Thuc-Huy Duong, Duc-Dung Pham, Hoang-Anh Pham, Van-Kieu Nguyen, Thi-Phuong Nguyen, Huu-Hung Nguyen, Ngoc-Hong Nguyen, Pornpat Sam-Ang, Kiettipum Phontree, Jirapast Sichaem. Design and synthesis of new lupeol derivatives and their α-glucosidase inhibitory and cytotoxic activities. Natural product research. 2022 Jan;36(1):1-7

Mesh Tags

Substances

PMID: 32378438

search → result