Hypolipidemic effects in monkeys of ML-236B, a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase

Abstract
The fungal metabolite ML-236B from Penicillium citrinum, a competitive inhibitor of 3-hydroxy-3-methylglutaryl CoA reductase, was effective in lowering serum cholesterol levels in cynomolgus monkeys at doses of 20-50 mg/kg per day. Levels of serum phospholipids and triglycerides were not significantly changed by the administration of the drug. Of the serum lipoprotein fractions a .beta.-lipoprotein corresponding to low density lipoprotein was preferentially reduced by the drug treatment. Fecal excretion of neutral sterols was unaffected, but that of bile acids was slightly elevated by the administration of ML-236B.