Beitz J, Riedel A, Beitz A, Giessler C, Kittel A, Mest H J
Department of Pharmacology and Toxicology, School of Medicine, Martin Luther University, Halle, G.D.R.
J Lipid Mediat. 1991 Mar-Apr;3(2):177-86.
The administration of the trapidil derivative AR 12465 (5 mg/kg body weight) intraperitoneally to hypercholesterolemic guinea pigs caused a stronger reduction in serum total cholesterol (TC) than trapidil (20 mg/kg, i.p.) or a vehicle injection (saline with 5% ethanol i.p.). The stronger reduction of TC is caused by a lower level in the sum of all beta-migrating lipoproteins and an enhanced level of high-density lipoprotein. The levels of free and esterified cholesterol were not changed in kidney and left cardiac ventricle, but significantly enhanced (P less than 0.05) in the liver of all groups fed a cholesterol-rich diet. The elevation in liver cholesterol was higher in the group treated with AR 12456 than in the group treated with trapidil or with vehicle. The treatment with AR 12456 diminished the ratio TXB2/6-keto-PGF1 alpha for the capacity of aorta to form these prostanoids. In conclusion, our data show that AR 12456 has a strong antilipidemic action in guinea pigs fed a cholesterol-rich diet.
给高胆固醇血症豚鼠腹腔注射曲匹地尔衍生物AR 12465（5毫克/千克体重），与注射曲匹地尔（20毫克/千克，腹腔注射）或溶剂（含5%乙醇的生理盐水，腹腔注射）相比，能更显著地降低血清总胆固醇（TC）。TC的更显著降低是由于所有β迁移脂蛋白总和水平降低以及高密度脂蛋白水平升高所致。在喂食富含胆固醇饮食的所有组中，肾脏和左心室中游离胆固醇和酯化胆固醇的水平未发生变化，但肝脏中的水平显著升高（P<0.05）。AR 12456治疗组肝脏胆固醇的升高幅度高于曲匹地尔治疗组或溶剂治疗组。AR 12456治疗降低了主动脉形成这些前列腺素的TXB2/6-酮-PGF1α比值。总之，我们的数据表明，AR 12456对喂食富含胆固醇饮食的豚鼠具有强大的抗血脂作用。
