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氯取代对含钒配合物降低糖尿病高血糖的作用及其通透性和细胞毒性。

Effect of the chloro-substitution on lowering diabetic hyperglycemia of vanadium complexes with their permeability and cytotoxicity.

机构信息

Department of Chemistry, Yunnan University, Kunming 650091, China.

出版信息

Eur J Med Chem. 2010 Dec;45(12):6077-84. doi: 10.1016/j.ejmech.2010.10.013. Epub 2010 Oct 16.

Abstract

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.

摘要

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。

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