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A novel PTP1b inhibitor vanadium-flavone complex: synthesis and pharmacodynamic evaluation in streptozotocin-induced diabetic mice


Indexed by:期刊论文

First Author:Duan, Liying

Co-author:Ye, Junwei,Sun, Wenlong,Wang, Shaoning,Gong, Wei-tao,Dong, Yuesheng,Ning, Guiling

Date of Publication:2017-09-01


Included Journals:SCIE、Scopus



Page Number:1863-1870

ISSN No.:1054-2523

Key Words:Oxide-vanadium; Baicalein; PTP1b inhibitor; Diabetic mice; Diabetes complications

Abstract:Protein tyrosine phosphatase 1b is a negative regulator of insulin action and is emerging as a potential drug target for type 2 diabetes mellitus. A novel protein tyrosine phosphatase 1b inhibitor vanadium-flavone complex, bis(5,6,7-trihydroxyflavone)-oxovanadium, was synthesized and characterized by mass spectrometer, inductively coupled plasma, infrared, ultraviolet, electron paramagnetic resonance, X-ray photoelectron spectroscopy and thermal gravity analysis. Bis(5,6,7-trihydroxyflavone)oxovanadium showed good anti-diabetic effect in streptozocin -induced diabetic mice without gastrointestinal stimulation and induction of hypoglycemia in normoglycemic mice. In vitro, the protein tyrosine phosphatase 1b inhibition activity of bis(5,6,7-trihydroxyflavone)-oxovanadium was enhanced after storage, during which bis(5,6,7-trihydroxyflavone)-oxovanadium could be decomposed gradually and the concentration of VO2+ would gradually increase. In vivo, baicalein not only transports VO2+ to the target organ, but also improves the morphology and function of pancreatic islets via its anti-inflammation activity. Thus bis(5,6,7-trihydroxyflavone)-oxovanadium is a promising potential drug for the treatment of type 2 diabetes mellitus.

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