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

被引：16

作者：

Hoang-Vinh-Truong Phan ^{[1
]}

Thuc-Huy Duong ^{[1
]}

Duc-Dung Pham ^{[1
]}

Hoang-Anh Pham ^{[1
]}

Van-Kieu Nguyen ^{[2
,3
]}

Thi-Phuong Nguyen ^{[4
]}

Huu-Hung Nguyen ^{[5
]}

Ngoc-Hong Nguyen ^{[6
]}

Sam-ang, Pornpat ^{[7
]}

Phontre, Kiettipum ^{[8
]}

Sichaem, Jirapast ^{[9
]}

机构：

[1] Univ Educ, Fac Chem, Ho Chi Minh City, Vietnam

[2] Duy Tan Univ, Inst Fundamental & Appl Sci, Ho Chi Minh City, Vietnam

[3] Duy Tan Univ, Fac Nat Sci, Da Nang, Vietnam

[4] Nguyen Tat Thanh Univ, Fac Biotechnol, Ho Chi Minh City, Vietnam

[5] Van Lang Univ, Fac Environm & Biotechnol, Ho Chi Minh City, Vietnam

[6] Ind Univ Ho Chi Minh City, Ho Chi Minh City, Vietnam

[7] Pibulsongkram Rajabhat Univ, Fac Sci & Technol, Phitsanulok, Thailand

[8] Khon Kaen Univ, Fac Pharmaceut Sci, Div Pharmacognosy & Toxicol, Khon Kaen, Thailand

[9] Thammasat Univ, Fac Sci & Technol, Lampang Campus, Lampang, Thailand

来源：

NATURAL PRODUCT RESEARCH | 2022年 / 36卷 / 01期

关键词：

Lupeol derivative; alpha-glucosidase inhibition; cytotoxicity; SELECTIVE OXIDATION; LICHENS; FUNGI;

D O I：

10.1080/14786419.2020.1758095

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

A series of lupeol derivatives 2, 2a-2f, 2a-2h, 3a-3e, and 4a-4b were designed, synthesised and evaluated for their alpha-glucosidase inhibitory and cytotoxic activities. Among synthetic derivatives, lupeol analogues 2b and 2e containing a benzylidene chain exhibited the best activity against alpha-glucosidase and superior to the positive agent with the IC50 values of 29.4 +/- 1.33 and 20.1 +/- 0.91 mu M, 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 mu M, respectively. [GRAPHICS] .

引用

页码：1 / 7

页数：7

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