Hypolipidemic activity of o-(N-phthalimido)acetophenone in Sprague Dawley rats.
o-(N-Phthalimido)acetophenone has proven to be an effective hypolipidemic agent in rats at 20 mg/kg/day orally. The agent suppressed the activity of the rate-limiting enzyme of the liver involved in de novo synthesis of triglycerides. The synthetic rate-limiting enzyme for cholesterol esters was also inhibited by the drug in vivo. o-(N-Phthalimido)acetophenone lowered cholesterol in the liver and the aorta wall and generally caused an increase in phospholipids in body tissues. Serum lipoproteins were modulated by the drug with a decrease in cholesterol and triglycerides in the chylomicron, very low-density lipoproteins (VLDL), and low-density lipoproteins (LDL) and an increase in high-density lipoprotein (HDL) cholesterol. The phospholipid content was increased in the chylomicron, VLDL, and LDL fractions. In hyperlipidemic rats, o-(N-phthalimido)acetophenone lowered elevated blood lipid levels at 20 mg/kg/day orally after 3 weeks of administration. The hypolipidemic rat after drug treatment had a lower LDL cholesterol and a higher HDL cholesterol content, which is therapeutically desirable to protect against cardiovascular disease.
D000098:Acetophenones / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D001011:Aorta / Q000032:analysis; D001059:Apoproteins / Q000032:analysis; D005243:Feces / Q000032:analysis; D000960:Hypolipidemic Agents / Q000633:toxicity; D008055:Lipids / Q000097:blood*; D008074:Lipoproteins / Q000302:isolation & purification; D008099:Liver / Q000032:analysis; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D010797:Phthalimides / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D011919:Rats, Inbred Strains
D000098:Acetophenones; D001059:Apoproteins; D000960:Hypolipidemic Agents; D008055:Lipids; D008074:Lipoproteins; D010797:Phthalimides; C056304:O-(N-phthalimido)acetophenone