Hypolipidemic activity of 3-N-(1',8'-Naphthalimido)propionic acid in rodents.

3-N-(1',8'-Naphthalimido)propionic acid was synthesized and shown to effectively lower both serum cholesterol and triglyceride levels in rats and mice. In hyperlipidemic mice, serum lipid levels were lowered significantly, approaching normal levels of cholesterol and below normal levels of triglyceride. The serum lipid levels were reduced due to accelerated clearance of cholesterol via the biliary route as well as a lowering of available acetyl CoA in the cytoplasm for liver de novo cholesterol and triglyceride syntheses. The liver regulatory enzyme of fatty acid and triglyceride syntheses were depressed by drug treatment. Significant reduction of liver lipids as well as the lipid content of the lipoprotein fractions were observed. The agent possessed a safe therapeutic index when used as a hypolipidemic agent.