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Bis(allixinato)oxovanadium(IV) Complex Is a Potent Antidiabetic Agent:  Studies on Structure−Activity Relationship for a Series of Hydroxypyrone−Vanadium Complexes

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journal contribution
posted on 01.06.2006, 00:00 by Yusuke Adachi, Jiro Yoshida, Yukihiro Kodera, Akira Katoh, Jitsuya Takada, Hiromu Sakurai
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-hydroxy-4-pyronato)oxovanadium(IV) (1) complexes with VO(O4) 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.