Bernini F, Corsini A, Raiteri M, Soma M R, Paoletti R
Institute of Pharmacological Sciences, University of Milan, Italy.
J Hypertens Suppl. 1993 Mar;11(1):S61-6. doi: 10.1097/00004872-199303001-00011.
To evaluate the effect of lacidipine on the major processes of atherogenesis.
Cell-culture methods were used to study the effect of lacidipine. Low-density lipoprotein (LDL) receptor expression and cholesterol esterification were evaluated in human skin fibroblasts and in mouse peritoneal macrophages, respectively. The effect of lacidipine on cellular proliferation was tested on aortic myocytes cultured from rat aorta.
Lacidipine did not affect LDL receptor expression, but it inhibited the ability of acetyl LDL to stimulate cholesterol esterification in macrophages by more than 95%. The drug inhibited cellular proliferation in a dose-dependent manner. This antiproliferative effect was confirmed in human femoral artery myocytes. In accord with the inhibitory effect on cellular growth, preliminary in vivo studies suggest that lacidipine may reduce neointimal formation induced by perivascular manipulation of the carotid artery in hypercholesterolemic rabbit.
Our results indicate that lacidipine may be antiatherosclerotic through an effect on the major processes involved in atheroma formation.
评估拉西地平对动脉粥样硬化形成主要过程的影响。
采用细胞培养方法研究拉西地平的作用。分别在人皮肤成纤维细胞和小鼠腹腔巨噬细胞中评估低密度脂蛋白（LDL）受体表达及胆固醇酯化情况。在从大鼠主动脉培养的主动脉肌细胞上测试拉西地平对细胞增殖的影响。
拉西地平不影响LDL受体表达，但它抑制乙酰LDL刺激巨噬细胞胆固醇酯化的能力达95%以上。该药物以剂量依赖方式抑制细胞增殖。这种抗增殖作用在人股动脉肌细胞中得到证实。与对细胞生长的抑制作用一致，初步体内研究表明拉西地平可能减少高胆固醇血症兔颈动脉血管周围操作诱导的新生内膜形成。
我们的结果表明，拉西地平可能通过对动脉粥样硬化形成所涉及的主要过程产生影响而具有抗动脉粥样硬化作用。
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