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Eur J Med Chem. 2019 Sep 15;178:108-115. doi: 10.1016/j.ejmech.2019.05.083. Epub 2019 May 30.

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

Author information

1
Key Laboratory of Industrial Fermentation Microbiology of Ministry of Education, China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Tianjin University of Science and Technology, Tianjin, 300457, China.
2
Key Laboratory of Industrial Fermentation Microbiology of Ministry of Education, China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Tianjin University of Science and Technology, Tianjin, 300457, China; Sorbonne Université, Institut Parisien de Chimie Moléculaire, UMR CNRS 8232, 4 place Jussieu, 75005, Paris, France. Electronic address: yongmin.zhang@upmc.fr.
3
Key Laboratory of Industrial Fermentation Microbiology of Ministry of Education, China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Tianjin University of Science and Technology, Tianjin, 300457, China. Electronic address: sunhua@tust.edu.cn.

Abstract

As dual regulators, the PTP-1B signaling pathway and α-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-3β 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 α-glucosidase in vitro, it could deglycosylated in vivo to diosmetin to function as an α-glucosidase inhibitor. Taken together, these results led to the identification of the natural flavonoids 1-6 from C. morifolium as dual regulators of α-glucosidase and the PTP-1B signaling pathway, suggesting their potential application as new oral anti-diabetic drugs or functional food ingredients.

KEYWORDS:

Chrysanthemum morifolium; Diabetes; Flavonoid; PTP-1B signaling; α-Glucosidase

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