Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 11, Pages 3251-3256Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm060229a
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There is an urgent medical need for orally effective drugs to replace insulin injections for the treatment of diabetes mellitus. Vanadium complexes with insulin-mimetic activities have recently been proposed as candidates as new antidiabetic drugs. Following in vitro and in vivo studies on a group of bis(3-hydroxy4-pyronato) oxovanadium(IV) (1) complexes with VO(O-4) coordination mode, bis(allixinato) oxovanadium( IV) (3) which contains allixin, a garlic component, was found to be the most potent antidiabetic agent among them. Complex 3 with a high in vitro insulin-mimetic activity in terms of both free fatty acid (FFA)release inhibitory and glucose-uptake enhancing activities in isolated rat adipocytes exhibited a high hypoglycemic effect in type 1 diabetic model mice by both intraperitoneal injections and oral administrations. Complex 3 is thus proposed to be one of the most effective candidates for antidiabetic therapy.
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