Design and synthesis of new lupeol derivatives and their α-glucosidase inhibitory and cytotoxic activities. Issue 1 (22nd December 2021)

• Record Type: Journal Article
• Authors: Phan, Hoang-Vinh-Truong; Duong, Thuc-Huy; Pham, Duc-Dung; Pham, Hoang-Anh; Nguyen, Van-Kieu; Nguyen, Thi-Phuong; Nguyen, Huu-Hung; Nguyen, Ngoc-Hong; Sam-ang, Pornpat; Phontree, Kiettipum; Sichaem, Jirapast
• Is Part Of: Natural product research. Volume 36:Issue 1(2022)
• Page Start: 1
• Page End: 7
• Publication Date: 2021-12-22
• Subjects: Lupeol derivative -- α-glucosidase inhibition -- cytotoxicity; Natural products -- Periodicals; Natural products -- Research -- Periodicals; Biological Factors -- Periodicals; Biological Products -- Periodicals; 547
• DOI: 10.1080/14786419.2020.1758095
• Languages: English
• ISSNs: 1478-6419

Abstract

Abstract: 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. Graphical Abstract: