New insights into the biological activities of Chrysanthemum morifolium: Natural flavonoids alleviate diabetes by targeting α-glucosidase and the PTP-1B signaling pathway

被引：49

作者：

Chen, Mingzhu ^{[1
]}

Wang, Kaili ^{[1
]}

Zhang, Yinan ^{[1
]}

Zhang, Mengdi ^{[1
]}

Ma, Yujiao ^{[1
]}

Sun, Haifeng ^{[1
]}

Jin, Zongxin ^{[1
]}

Zheng, Hang ^{[1
]}

Jiang, He ^{[1
]}

Yu, Peng ^{[1
]}

Zhang, Yongmin ^{[1
,2
]}

Sun, Hua ^{[1
]}

机构：

[1] Tianjin Univ Sci & Technol, China Int Sci & Technol Cooperat Base Food Nutr S, Minist Educ, Key Lab Ind Fermentat Microbiol, Tianjin 300457, Peoples R China

[2] Sorbonne Univ, Inst Parisien Chim Mol, UMR CNRS 8232, 4 Pl Jussieu, F-75005 Paris, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2019年 / 178卷

基金：

中国国家自然科学基金;

关键词：

Chrysanthemum morifolium; Flavonoid; Diabetes; alpha-Glucosidase; PTP-1B signaling; IN-VITRO; SELECTIVITY;

D O I：

10.1016/j.ejmech.2019.05.083

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

As dual regulators, the PTP-1B signaling pathway and alpha-glucosidase slow glucose release and increase the degree of insulin sensitivity, representing a promising therapeutic target for type 2 diabetes. In this study, we systematically examined the in vivo and in vitro anti-diabetic activities of natural flavonoids 1-6 from Chrysanthemum morifolium. Flavonoids 1-6 increased glucose consumption-promoting activity and the phosphorylation of GSK-3 beta and Akt, and decreased PTP-1B protein level along with slightly inhibitory activity of the PTP-1B enzyme. Moreover, flavonoids 1-2 treatment induced insulin secretion in INS-1 cells. Besides, in vivo study revealed that flavonoids 2 and 5 demonstrated potent anti hyperglycemic and anti-hyperlipidemic activity, and improved maltose and glucose tolerance. Although flavonoid 2 exhibited lower inhibitory activity against alpha-glucosidase in vitro, it could deglycosylated in vivo to diosmetin to function as an alpha-glucosidase inhibitor. Taken together, these results led to the identification of the natural flavonoids 1-6 from C. morifolium as dual regulators of alpha-glucosidase and the PTP-1B signaling pathway, suggesting their potential application as new oral anti-diabetic drugs or functional food ingredients. (C) 2019 Elsevier Masson SAS. All rights reserved.

引用

页码：108 / 115

页数：8

共 21 条

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