Bis(allixinato)oxovanadium(IV) complex is a potent antidiabetic agent: Studies on structure-activity relationship for a series of hydroxypyrone-vanadium complexes
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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DOI：
10.1021/jm060229a
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发表时间：
2006-06-01
影响因子：
7.3
通讯作者：
Sakurai, Hiromu
中科院分区：
文献类型：
--
作者：
Adachi, Yusuke;Yoshida, Jiro;Sakurai, Hiromu
医学上迫切需要口服有效的药物来代替胰岛素注射治疗糖尿病。具有类胰岛素活性的钒酸盐配合物最近被提出作为新的抗糖尿病药物的候选者。通过对一组VO（O-4）配位模式的双（3-羟基-4-吡喃）氧钒（IV）（1）配合物的体内外研究，发现其中含有大蒜素的双（大蒜素）氧钒（IV）（3）是最有效的抗糖尿病药物。配合物3具有高的体外胰岛素模拟活性，在分离的大鼠脂肪细胞中的游离脂肪酸（FFA）释放抑制和葡萄糖摄取增强活性，通过腹腔注射和口服给药在1型糖尿病模型小鼠中表现出高的降血糖作用。因此，配合物3被认为是抗糖尿病治疗的最有效的候选者之一。
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.