Shirai K, Ishikawa Y, Nishide T, Sasaki N, Murano S, Sato A, Matsuoka N, Saito Y, Yoshida S
Tohoku J Exp Med. 1984 Jun;143(2):231-8. doi: 10.1620/tjem.143.231.
Atherosclerotic lesions were formed in the aorta of rats given a high cholesterol diet containing propylthiouracil (PTU) and vitamin D2 (atherogenic diet) for 8 weeks. The effects of niceritrol (pentaerythritol tetranicotinate), which lower the plasma lipid level, on lipid metabolism in the arterial wall of the atherosclerotic rats were studied. Niceritrol significantly decreased the plasma cholesterol level of atherosclerotic rats, which was 823 mg/100 ml, or about ten times that of control rats. On treatment with niceritrol, the cholesterol level was reduced most in the very low density lipoprotein (VLDL) fraction (d less than 1.006). Heparin-releasable lipoprotein lipase activity in epididymal adipose tissue, lipoprotein lipase activity in post-heparin plasma, and VLDL-triolein hydrolyzing activity in adipose tissue stromal vessels were all higher in niceritrol-treated atherosclerotic rats. Of the enzymes in the arterial wall concerned with cholesterol ester metabolism, acid cholesterol esterase activity was decreased in atherosclerotic rats, while niceritrol treatment increased this activity. The ratio of acyl-CoA cholesterol acyltransferase activity (ACAT) to neutral cholesterol esterase activity was higher in atherosclerotic rats than in control rats, but was lower in niceritrol-treated rats than in atherosclerotic rats. From these results, it is concluded that niceritrol modifies enzyme activities in such a way as to reduce the cholesterol ester content of the arterial wall and lower plasma VLDL and LDL cholesterol levels.
给大鼠喂食含丙硫氧嘧啶（PTU）和维生素D2的高胆固醇饮食（致动脉粥样化饮食）8周后，其主动脉中形成了动脉粥样硬化病变。研究了能降低血浆脂质水平的烟浪丁（季戊四醇四烟酸酯）对动脉粥样硬化大鼠动脉壁脂质代谢的影响。烟浪丁显著降低了动脉粥样硬化大鼠的血浆胆固醇水平，该水平为823毫克/100毫升，约为对照大鼠的10倍。用烟浪丁治疗后，极低密度脂蛋白（VLDL）部分（密度小于1.006）的胆固醇水平降低最多。在接受烟浪丁治疗的动脉粥样硬化大鼠中，附睾脂肪组织中肝素可释放的脂蛋白脂肪酶活性、肝素后血浆中的脂蛋白脂肪酶活性以及脂肪组织基质血管中的VLDL - 三油精水解活性均较高。在动脉壁中与胆固醇酯代谢有关的酶中，动脉粥样硬化大鼠的酸性胆固醇酯酶活性降低，而烟浪丁治疗可增加该活性。动脉粥样硬化大鼠中酰基辅酶A胆固醇酰基转移酶活性（ACAT）与中性胆固醇酯酶活性的比值高于对照大鼠，但在接受烟浪丁治疗的大鼠中低于动脉粥样硬化大鼠。从这些结果可以得出结论，烟浪丁以降低动脉壁胆固醇酯含量以及降低血浆VLDL和LDL胆固醇水平的方式改变酶活性。
