Franzoni Ferdinando, Santoro Gino, Regoli Francesco, Plantinga Yvonne, Femia Francesca R, Carpi Angelo, Galetta Fabio
Department of Internal Medicine, University of Pisa, Via Roma, 67, 56100 Pisa, Italy.
Biomed Pharmacother. 2004 Oct;58(8):423-6. doi: 10.1016/j.biopha.2004.08.003.
Amlodipine has been reported to improve endothelial function in patients with arterial hypertension and to significantly limit the progression of carotid atherosclerosis. The aim of this study was to assess the total antioxidant activity of amlodipine. We measured the in vitro antioxidant activity of amlodipine as its ability to antagonize the oxidation of alpha-keto-gamma-methiolbutyric acid by both hydroxyl and peroxyl radicals. The results are expressed as Total Oxyradical Scavenging Capacity (TOSC) units. Reduced glutathione, uric acid and trolox were used as the reference antioxidants. Amlodipine showed an efficiency as scavenger of peroxyl radicals (TOSC: 5945 +/- 544 units/mg) significantly higher (>50%, P <0.001) than that of GSH (2733 +/- 636 units/mg), and 70% lower (P < 0.0001) than the value obtained with uric acid (18144 +/- 696 units/mg) and trolox (17522 +/- 734 units/mg). Of interest, the scavenging capacity of amlodipine towards hydroxyl radicals (1455 +/- 154 units/mg) was 320% higher (P < 0.00001) than that of GSH (358 +/- 112 units/mg), 20% higher than that of uric acid (1198 +/- 121 units/mg), and 100% higher than that of trolox (759 +/- 143 units/mg). Amlodipine has intrinsic antioxidant activity with both anti-hydroxyl and anti-peroxyl radicals activity.
据报道，氨氯地平可改善动脉高血压患者的内皮功能，并显著限制颈动脉粥样硬化的进展。本研究的目的是评估氨氯地平的总抗氧化活性。我们测量了氨氯地平的体外抗氧化活性，即其拮抗羟基自由基和过氧自由基氧化α-酮-γ-甲硫基丁酸的能力。结果以总氧自由基清除能力（TOSC）单位表示。还原型谷胱甘肽、尿酸和曲克芦丁用作参考抗氧化剂。氨氯地平作为过氧自由基清除剂的效率（TOSC：5945±544单位/毫克）显著高于谷胱甘肽（2733±636单位/毫克）（>50%，P<0.001），比尿酸（18144±696单位/毫克）和曲克芦丁（17522±734单位/毫克）获得的值低70%（P<0.0001）。有趣的是，氨氯地平对羟基自由基的清除能力（1455±154单位/毫克）比谷胱甘肽（358±112单位/毫克）高320%（P<0.00001），比尿酸（1198±121单位/毫克）高20%，比曲克芦丁（759±143单位/毫克）高100%。氨氯地平具有内在的抗氧化活性，兼具抗羟基自由基和抗过氧自由基活性。
