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论文类型：期刊论文

发表时间：2017-09-01

发表刊物：MEDICINAL CHEMISTRY RESEARCH

收录刊物：SCIE、Scopus

卷号：26

期号：9

页面范围：1863-1870

ISSN号：1054-2523

关键字：Oxide-vanadium; Baicalein; PTP1b inhibitor; Diabetic mice; Diabetes complications

摘要：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.