Analogues of xanthones- -Chalcones and bis-chalcones as α-glucosidase inhibitors and anti-diabetes candidates

被引：84

作者：

Cai, Chao-Yun ^{[1
]}

Rao, Li ^{[1
]}

Rao, Yong ^{[2
]}

Guo, Jin-Xuan ^{[1
]}

Xiao, Zhi-Zun ^{[1
]}

Cao, Jing-Yu ^{[1
]}

Huang, Zhi-Shu ^{[2
]}

Wang, Bo ^{[1
]}

机构：

[1] Sun Yat Sen Univ, Sch Chem, 135 Xingang West Rd, Guangzhou 510275, Guangdong, Peoples R China

[2] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510080, Guangdong, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2017年 / 130卷

基金：

中国国家自然科学基金;

关键词：

alpha-glucosidase inhibitors; Chalcones; Bis-chalcones; Noncompetitive; SYNERGETIC INHIBITION; DERIVATIVES; MANAGEMENT; ANTICANCER; GENISTEIN; INSIGHT;

D O I：

10.1016/j.ejmech.2017.02.007

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

Two series of compounds (chalcones and bis-chalcones) were designed, synthesized, and evaluated as aglucosidase inhibitors (AGIs) with 1-deoxynojirimycin as positive control in vitro. Most of the compounds with two or four hydroxyl groups showed better inhibitory activities than 1-deoxynojirimycin towards aglucosidase with noncompetitive mechanism. Moreover, most of the hydroxy bis-chalcones exhibit good a-glucosidase inhibitory activities in enzyme test. Inspiringly, bis-chalcones 2g (at 1 mu M concentration) has stronger effect than 1-deoxynojirimycin on reducing the glucose level in HepG-2 cells (human liver cancer cell line). (C) 2017 Elsevier Masson SAS. All rights reserved.

引用

页码：51 / 59

页数：9

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