Yao K, Ina Y, Nagashima K, Ohmori K, Ohno T
Drug Development Research Laboratories, Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd., Japan.
Biol Pharm Bull. 2000 Jun;23(6):766-9. doi: 10.1248/bpb.23.766.
We studied the antioxidant activities of calcium antagonists against autoxidation in rat brain homogenates. The homogenates were incubated for 30 min at 37 degrees C with or without a calcium antagonist and subsequently assayed for lipid peroxide content. Percent inhibition of the lipid peroxidation was used as an index of the antioxidant effect. Dihydropyridine calcium antagonists exhibited concentration-dependent (3-300 micromol/l) inhibitory effects against lipid peroxidation. The relative order of antioxidant potency and associated IC50 values (micromol/l) of the calcium antagonists for inhibition of the lipid peroxidation were as follows: nifedipine (51.5)>barnidipine (58.6)>benidipine (71.2)>nicardipine (129.3)>amlodipine (135.5)>nilvadipine (167.3)>nitrendipine (252.1)>> diltiazem (>300)=verapamil (>300). These results suggest that some dihydropyridine calcium antagonists show antioxidant properties. The antioxidant effects of the calcium antagonists may contribute to their pharmacological actions.
我们研究了钙拮抗剂对大鼠脑匀浆自氧化的抗氧化活性。将匀浆在37℃下孵育30分钟，分别添加或不添加钙拮抗剂，随后测定脂质过氧化物含量。脂质过氧化的抑制百分比用作抗氧化作用的指标。二氢吡啶类钙拮抗剂对脂质过氧化表现出浓度依赖性（3 - 300微摩尔/升）抑制作用。钙拮抗剂抑制脂质过氧化的抗氧化效力相对顺序及相关IC50值（微摩尔/升）如下：硝苯地平（51.5）>巴尼地平（58.6）>贝尼地平（71.2）>尼卡地平（129.3）>氨氯地平（135.5）>尼伐地平（167.3）>尼群地平（252.1）>>地尔硫卓（>300）=维拉帕米（>300）。这些结果表明，一些二氢吡啶类钙拮抗剂具有抗氧化特性。钙拮抗剂的抗氧化作用可能有助于其药理作用。
