Antihyperlipidemic Activity of Phthalimide Analogues in Rodents

Abstract

□ Phthalimide analogues have been shown to effectively lower serum cholesterol and triglyceride levels in rats and mice. The mode of action of these agents was not to suppress the appetite of animals, but rather to reduce the activities of key enzymes in the early synthesis of liver cholesterol and fatty acids in the triglyceride pathway. Phthalimide analogues were effective in accelerating biliary excretion of cholesterol and blocking its absorption from the gut. After 16 days dosing, it was evident that higher levels of lipids were being excreted than in control mice. The major serum lipoprotein fractions were reduced in cholesterol, triglyceride, and neutral lipid content, but not phospholipid content in rats after 14 days of administration.