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首页> 外文期刊>Life sciences >Troglitazone-binding to Ldl and its glycated modifications - Its role in cell-catalysed and Cu-mediated Ldl-oxidation
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Troglitazone-binding to Ldl and its glycated modifications - Its role in cell-catalysed and Cu-mediated Ldl-oxidation

机译：曲格列酮结合Ldl及其糖基化修饰-在细胞催化和Cu介导的Ldl氧化中的作用

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摘要

Troglitazone (T), an anti-diabetic drug improving insulin resistance, was studied as to its inhibition of copper ion-catalysed oxidation of native, glycated and glycoxidated low-density lipoprotein (LDL). A dose-dependent inhibition was noted in the concentration range 40-160 mu g/ml. An almost complete inhibition of oxidation (2-8 h), as monitored by the formation of thiobarbituric acid-reactive substances, was observed for both native and glycated LDL at a concentration of 160 mu g/ml T, while the maximal inhibition for glycoxidated LDL amounted only to 60% at this concentration of the drug. This is reflected by differences in the affinity of the drug for the different types of LDL modification: While the binding of T both to native or glycated LDL increased linearly with increasing T concentration and was not saturable in the concentration range rested (0-160 mu g/ml), binding of the drug to glycoxidated LDL was already nearly saturated at 10 mu g/ml. The nearly complete inhibitory action of T towards oxidation of native and glycated LDL was lost, however, upon increasing the total oxidation time to 24 h. In human umbilical vein endothelial cell-mediated oxidation of LDL, T at a concentration of 20 mu g/ml significantly reduced formation of oxidation-dependent fluorescent chromophores and liberation of 8-epi-PGF(2 alpha). In contrast, generation of thiobarbituric acid-reactive substances was not significantly inhibited. As opposed to copper-mediated LDL-oxidation, different binding of T to LDL-modifications does not govern inhibition of human umbilical vein endothelial cell-mediated LDL-oxidation. (C) 2000 Elsevier Science Inc. All rights reserved. [References: 34]
机译：曲格列酮（T）是一种抗糖尿病药物，可改善胰岛素抵抗，其对铜离子催化的天然，糖基化和糖化低密度脂蛋白（LDL）的氧化抑制作用得到了研究。在40-160μg/ ml的浓度范围内观察到剂量依赖性抑制。天然和糖化低密度脂蛋白在160μg / ml T的浓度下都观察到几乎完全抑制氧化作用（2-8小时），这是通过硫代巴比妥酸反应性物质的形成来监测的，而对糖化氧化的抑制作用最大。在这种药物浓度下，LDL仅占60％。药物对不同类型的LDL修饰的亲和力差异反映了这一点：尽管T与天然或糖化LDL的结合随T浓度的增加而线性增加，并且在静止的浓度范围内（0-160微米）不饱和10克/毫升），药物与糖氧化LDL的结合已经接近饱和，达到10微克/毫升。然而，在将总氧化时间增加至24小时后，T对天然和糖基LDL氧化的几乎完全抑制作用消失了。在人脐静脉内皮细胞介导的LDL氧化中，浓度为20μg / ml的T显着减少了氧化依赖性荧光发色团的形成和8-epi-PGF（2 alpha）的释放。相反，对硫代巴比妥酸反应性物质的产生没有受到明显的抑制。与铜介导的LDL-氧化相反，T与LDL-修饰的不同结合不能控制对人脐静脉内皮细胞介导的LDL-氧化的抑制。 （C）2000 Elsevier Science Inc.保留所有权利。 [参考：34]

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