Marquie G
Eur J Pharmacol. 1977 Sep 1;45(1):1-6. doi: 10.1016/0014-2999(77)90051-6.
Pretreatment of rabbits with Benfouorex (780 SE) 50 mg/kg p.o. for 10 days strongly inhibited the incorporation of a 20 muCi tracer dose of 4-14C-cholesterol (given i.v. 24 h earlier) into various segments of the aorta. Incorporation of specific activity into the liver, intestine, lung or plasma was not affected. 1 h after i.v. injection of a 100 muCi tracer dose of 2-14C-acetate, a significant reduction in the radioactivity of total lipids of the aorta and liver was seen in rabbits pretreated with 780 SE. The inhibition of acetate incorporation into arterial lipids was observed in all lipid fractions (i.e. free fatty acids, free and esterfied cholesterol, phospholipids and especially triglycerides). Incorporation of acetate into triglyceride fractions of liver and intestine and into hepatic cholesterol was also significantly decreased. The results indicate that 780 SE may have anti-atherogenic properties which could be valuable in the clinical treatment of atherosclerosis.
用苯氟雷司(780 SE)50毫克/千克口服给药对兔子进行预处理10天,可强烈抑制20微居里示踪剂量的4-¹⁴C-胆固醇(24小时前静脉注射)掺入主动脉的各个节段。掺入肝脏、肠道、肺或血浆中的比活性不受影响。静脉注射100微居里示踪剂量的2-¹⁴C-醋酸盐1小时后,在用780 SE预处理的兔子中,主动脉和肝脏总脂质的放射性显著降低。在所有脂质组分(即游离脂肪酸、游离和酯化胆固醇、磷脂,尤其是甘油三酯)中均观察到醋酸盐掺入动脉脂质的抑制。醋酸盐掺入肝脏和肠道的甘油三酯组分以及肝脏胆固醇中的量也显著减少。结果表明,780 SE可能具有抗动脉粥样硬化特性,这在动脉粥样硬化的临床治疗中可能具有重要价值。