In Vitro Antioxidant Activity of Calcium Antagonists against LDL Oxidation Compared with α-Tocopherol
In Vitro Antioxidant Activity of Calcium Antagonists against LDL Oxidation Compared with α-Tocopherol
复制标题
与 α-生育酚相比，钙拮抗剂对 LDL 氧化的体外抗氧化活性
DOI：
10.1006/bbrc.1994.2396
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发表时间：
1994
影响因子：
3.1
通讯作者：
W. Vetter
中科院分区：
文献类型：
--
作者：
E. Lupo;R. Locher;B. Weisser;W. Vetter
摘要 通过测量二烯形成和 TBARS 含量，比较钙拮抗剂（维拉帕米、地尔硫卓、硝苯地平、氨氯地平、伊拉地平或拉西地平）和 α-生育酚对铜诱导的 LDL（0.25 mg/ml）氧化的剂量依赖性（1、5、10、50 μM）抗氧化活性。对于地尔硫卓，未发现抗氧化作用，而其他钙拮抗剂和 α-生育酚至少在 10 和 50 μM 浓度下具有抗氧化活性：α-生育酚 > 拉西地平 > 硝苯地平 > 伊拉地平、维拉帕米、氨氯地平。此外，α-生育酚和拉西地平在 1 和 5 μM 时能够显着减弱 LDL 氧化。这些结果表明钙拮抗剂的体外抗氧化活性，尤其是二氢吡啶型拮抗剂，对强亲脂性拉西地平具有最大活性。这可能是钙拮抗剂的一种可能的抗动脉粥样硬化机制，因为氧化修饰增强了低密度脂蛋白的致动脉粥样硬化潜力。
Abstract The dose-dependent (1, 5, 10, 50 μM) antioxidative activity of calcium antagonists (verapamil, diltiazem, nifedipine, amlodipine, isradipine or lacidipine) and α-tocopherol against copper-induced LDL (0.25 mg/ml) oxidation was compared by measuring the diene formation and the content of TBARS. For diltiazem no antioxidant effect could be found, whereas the other calcium antagonists and α-tocopherol have demonstrated antioxidant activity at least at concentrations of 10 and 50 μM: α-tocopherol > lacidipine > nifedipine > isradipine, verapamil, amlodipine. Additionally, α-tocopherol and lacidipine were able to attenuate LDL-oxidation significantly at 1 and 5 μM These results indicate in vitro antioxidative activity of calcium antagonists especially from the dihydropyridine-type with greatest activity for the strongly lipophilic lacidipine. This might be one possible antiatherogenic mechanism of calcium antagonists, since oxidative modification enhances the atherogenic potential of LDL.