钙通道阻滞剂对超氧阴离子的影响。

The influence of calcium channel blockers on superoxide anions.

作者信息

Shridi F, Robak J

机构信息

Department of Pharmacology, Copernicus Academy of Medicine, Cracow, Poland.

出版信息

Pharmacol Res Commun. 1988 Jan;20(1):13-21. doi: 10.1016/s0031-6989(88)80603-9.

DOI:10.1016/s0031-6989(88)80603-9

PMID:2836871

Abstract

Four calcium channel blockers were tested from the point of view of their influence on enzymic lipid oxidation and on generation of superoxide anions. All the compounds were found to be antioxidants as tested by the inhibition of NADPH-stimulated malonaldehyde formation from lipids. IC50 values were 60 microM for nifedipine; 1.1 microM for verapamil; 1.4 microM for fendiline and 20.6 microM for diltiazem. Only nifedipine scavenged superoxide anions both in an enzymic (xanthine:xanthine oxidase) and non-enzymic (phenazine methosulphate:NADH) generating system. IC50 values for this inhibition were about 2.5 times higher than for inhibition of formation of malonaldehyde. Nifedipine inhibited also xanthine oxidase-mediated formation of uric acid.

摘要

从对酶促脂质氧化和超氧阴离子生成的影响角度，测试了四种钙通道阻滞剂。通过抑制由脂质产生的NADPH刺激的丙二醛形成进行测试，发现所有化合物均为抗氧化剂。硝苯地平的IC50值为60微摩尔；维拉帕米为1.1微摩尔；芬地林为1.4微摩尔；地尔硫䓬为20.6微摩尔。只有硝苯地平在酶促（黄嘌呤：黄嘌呤氧化酶）和非酶促（吩嗪硫酸甲酯：NADH）生成系统中均能清除超氧阴离子。这种抑制的IC50值比抑制丙二醛形成的IC50值高约2.5倍。硝苯地平还抑制黄嘌呤氧化酶介导的尿酸形成。