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一种新的水杨酸衍生曲酸氧钒配合物:合成、表征和抗糖尿病治疗潜力。

A new salicylic acid-derivatized kojic acid vanadyl complex: synthesis, characterization and anti-diabetic therapeutic potential.

机构信息

State Key Laboratories of Natural and Biomimetic Drugs and Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, PR China.

出版信息

J Inorg Biochem. 2011 Aug;105(8):1081-5. doi: 10.1016/j.jinorgbio.2011.05.008. Epub 2011 May 27.

Abstract

The molecular mechanisms of vanadium toxicity suggest that incorporation of antioxidant groups in the structure of vanadium complexes could be a preferable strategy in designing novel hypoglycemic vanadium complexes with proper efficacy and safety. By conjugating a pyrone skeleton to provide a coordination group and antioxidative motifs, we synthesized a novel complex of bis ((5-hydroxy-4-oxo-4H-pyran-2-yl) methyl 2-hydroxy- benzoatato) oxovanadium (IV) (BSOV). Evaluation of the anti-diabetic effects of BSOV using streptozotocin (STZ)-induced diabetic rats with bis (maltolato) oxovanadium (BMOV) as a positive control showed that BSOV effectively lowered blood glucose level, ameliorated damages of hepatic and renal function in diabetic rats and improved lipid metabolism. The signs of potential alteration of renal function caused by BSOV and BMOV were observed and are discussed. Overall, the experimental results suggest BSOV as a potent hypoglycemic agent and further studies using this strategy for anti-diabetic agents.

摘要

钒毒性的分子机制表明,在设计具有适当疗效和安全性的新型降糖钒配合物时,在钒配合物的结构中加入抗氧化基团可能是一种更可取的策略。通过将吡喃酮骨架连接起来提供配位基团和抗氧化基序,我们合成了一种新型的双((5-羟基-4-氧代-4H-吡喃-2-基)甲基 2-羟基-苯甲酸酯)氧化氧钒(IV)(BSOV)。用链脲佐菌素(STZ)诱导的糖尿病大鼠作为阳性对照,评价 BSOV 的抗糖尿病作用,结果表明 BSOV 能有效降低血糖水平,改善糖尿病大鼠的肝肾功能损伤,改善脂代谢。观察到并讨论了 BSOV 和 BMOV 引起的肾功能潜在改变的迹象。总的来说,实验结果表明 BSOV 是一种有效的降血糖药物,并进一步研究了这种策略在抗糖尿病药物中的应用。

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