N-（4-甲基苯基）二苯甲酰亚胺对斯普拉格-道利大鼠脂质代谢的影响。

The effects of N(4-methylphenyl)diphenimide on lipid metabolism of Sprague Dawley rats.

作者信息

Hall I H, Wong O T, Simlot R, Reynolds D J

机构信息

Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill 27599-7360.

出版信息

Pharm Res. 1992 Oct;9(10):1324-9. doi: 10.1023/a:1015817720101.

DOI:10.1023/a:1015817720101

PMID:1448433

Abstract

N(4-Methylphenyl)diphenimide proved to be an effective hypolipidemic agent in rats at 10 and 20 mg/kg/day. Both serum cholesterol and triglyceride levels were reduced significantly. Decreases in tissue lipids as well as VLDL cholesterol levels were observed. HDL-cholesterol was elevated even at 10 mg/kg/day. The agent was equally effective in hyperlipidemic diet-induced rats, lowering serum lipids and VLDL- and LDL-cholesterol while elevating HDL-cholesterol levels. The drug interfered with the incorporation of 3H-cholesterol and 3H-palmitic acid into chylomicrons, VLDL, and LDL. The two precursors were incorporated at a higher rate into HDL. 3H-Leucine was incorporated into chylomicrons, VLDL, and LDL at a higher rate, but not into HDL. Reduced uptake of the precursor for lipid synthesis was noted in tissues after treatment with the drug.

摘要

N-(4-甲基苯基)二苯甲酰亚胺在大鼠体内以10毫克/千克/天和20毫克/千克/天的剂量时被证明是一种有效的降血脂药物。血清胆固醇和甘油三酯水平均显著降低。观察到组织脂质以及极低密度脂蛋白胆固醇水平下降。即使在10毫克/千克/天的剂量下，高密度脂蛋白胆固醇也有所升高。该药物对高脂饮食诱导的大鼠同样有效，可降低血脂、极低密度脂蛋白和低密度脂蛋白胆固醇水平，同时提高高密度脂蛋白胆固醇水平。该药物干扰了3H-胆固醇和3H-棕榈酸掺入乳糜微粒、极低密度脂蛋白和低密度脂蛋白。这两种前体以更高的速率掺入高密度脂蛋白。3H-亮氨酸以更高的速率掺入乳糜微粒、极低密度脂蛋白和低密度脂蛋白，但不掺入高密度脂蛋白。用药治疗后，组织中脂质合成前体的摄取减少。