The hypolipidemic activity of 1-N-3-methylphthalimido-butan-3-semicarbazone in rodents.
The hypolipidemic activity of 1-N-3-methylphthalimido-butan-3-semicarbazone in rodents.
复制标题
1-N-3-甲基邻苯二甲酰亚胺基丁-3-缩氨基脲在啮齿动物中的降血脂活性。
DOI：
10.1023/a:1015965517279
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发表时间：
1989
影响因子：
3.7
通讯作者：
ChapmanJr,JM
中科院分区：
文献类型：
--
作者：
Wong,OT;Hall,IH;ChapmanJr,JM
1-N-（3-甲基苯二甲酰亚胺）丁-3-酮缩氨基脲对正常大鼠、小鼠和高血脂饮食诱导的小鼠均表现出较强的降血脂活性。该化合物降低组织脂质水平并增加胆固醇和甘油三酯的粪便排泄。给药2周后，调节血清脂蛋白水平，使极低密度脂蛋白（VLDL）和低密度脂蛋白（LDL）胆固醇浓度降低，高密度脂蛋白（HDL）胆固醇浓度升高至先前测试的环酰亚胺衍生物前所未有的水平。VLDL甘油三酯含量也降低。Hepaticin体外酶促研究表明，该化合物抑制了脂肪酸和胆固醇早期合成中的酶活性以及甘油三酯从头合成的调节酶。
l-N-(3-Methylphthalimido)butan-3-one semicarbazone demonstrated potent hypolipidemic activity in normal rats and mice and hyperlipidemic diet-induced mice. The compound decreased tissue lipid levels and increased the fecal excretion of cholesterol and triglycerides. After 2 weeks of administration, serum lipoprotein levels were modulated so that very low-density lipoprotein (VLDL) and low-density lipoprotein (LDL) cholesterol concentrations were reduced and high-density lipoprotein (HDL) cholesterol concentrations were elevated to levels unprecedented by the cyclic imide derivatives previously tested. The VLDL triglyceride content was also reduced. Hepaticin vitroenzymatic studies demonstrated that the compound suppressed the activity of enzymes in the early synthesis of fatty acids and cholesterol and the regulatory enzymes for the de novo synthesis of triglycerides.