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具有VO(O4)配位模式的氧钒基吡喃酮和吡啶酮配合物的胰岛素样作用的体外研究。

In vitro study of the insulin-like action of vanadyl-pyrone and -pyridinone complexes with a VO(O4) coordination mode.

作者信息

Rangel M, Tamura A, Fukushima C, Sakurai H

机构信息

CEQUP/Instituto de Ciencias Biomedicas de Abel Salazar, Universidade do Porto, Portugal.

出版信息

J Biol Inorg Chem. 2001 Feb;6(2):128-32. doi: 10.1007/s007750000180.

Abstract

The insulin-like action of a novel class of potential insulin-mimetic complexes was investigated in terms of free fatty acid (FFA) release from isolated rat adipocytes. Vanadyl complexes such as VO(ema)2 [(bis(2-ethyl-3-hydroxy-4-pyrone)VO], VO(mpp)2 [bis (3-hydroxy-2-methyl-4(1H)-pyridinone)VO], VO(dmpp)2 [bis(1,2-dimethyl-3-hydroxy-4(1H)-pyridinone)VO] and VO(empp)2 [bis(2-ethyl-3-hydroxy-1-methyl-4(1H)-pyridinone)VO] were tested together with vanadyl sulfate for comparison. The inhibitory effect of the vanadium complexes on FFA release, from rat adipocytes treated with epinephrine, is dependent on concentration and for that reason the results are reported in terms of the IC50 value, the 50% inhibition concentration. The results show that all the complexes have an inhibitory effect on FFA release and that two pyridinone complexes, VO(mpp)2 and VO(empp)2, have a significantly better insulin-mimetic activity than that of vanadyl sulfate.

摘要

根据从分离的大鼠脂肪细胞中释放游离脂肪酸(FFA)的情况,对一类新型潜在胰岛素模拟复合物的胰岛素样作用进行了研究。测试了钒酰配合物,如VO(ema)2 [双(2-乙基-3-羟基-4-吡喃酮)VO]、VO(mpp)2 [双(3-羟基-2-甲基-4(1H)-吡啶酮)VO]、VO(dmpp)2 [双(1,2-二甲基-3-羟基-4(1H)-吡啶酮)VO]和VO(empp)2 [双(2-乙基-3-羟基-1-甲基-4(1H)-吡啶酮)VO],并与硫酸氧钒进行比较。钒配合物对肾上腺素处理的大鼠脂肪细胞中FFA释放的抑制作用取决于浓度,因此结果以IC50值(50%抑制浓度)报告。结果表明,所有配合物均对FFA释放有抑制作用,且两种吡啶酮配合物VO(mpp)2和VO(empp)2的胰岛素模拟活性明显优于硫酸氧钒。

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