Department of Chemistry, Yunnan University, Kunming 650091, China.
Eur J Med Chem. 2010 Dec;45(12):6077-84. doi: 10.1016/j.ejmech.2010.10.013. Epub 2010 Oct 16.
The effect of the chloro-substitution of dinuclear vanadium (V) complexes on lowering diabetic hyperglycemia was evaluated. The in vivo tests for hypoglycemic activity show that complex 2 at the dose of 10.0 and 20.0 mg V kg(-1), could significantly decrease the blood glucose level. Importantly, our results the chloro substituent increased the insulin-enhancing properties of the complex 2. The two vanadium compounds had permeability above 10(-5) cm/s. It suggested that two complexes permeate via a passive diffusion mechanism. It was also suggested that two complexes has better good lipophilic properties. The cytotoxicity of two complexes on Caco-2 cells suggested the chlorine atom at C4 of complex 2 increased cytotoxicity for vanadium complexes.
我们评估了双核钒(V)配合物的氯取代基对降低糖尿病高血糖的影响。体内试验表明，配合物 2 在 10.0 和 20.0 mg V kg(-1)剂量下，能显著降低血糖水平。重要的是，我们的结果表明，氯取代基增加了配合物 2 的胰岛素增强特性。这两种钒化合物的透过率均高于 10(-5) cm/s。这表明两种配合物通过被动扩散机制渗透。这也表明两种配合物具有更好的亲脂性。两种配合物对 Caco-2 细胞的细胞毒性表明，配合物 2 中 C4 上的氯原子增加了钒配合物的细胞毒性。
