Inhibition of cholesterol synthesis by lovastatin tested on six human cell types in vitro.

Lovastatin (mevinolin) caused a strong and dose-dependent inhibition of cholesterol synthesis in six types of cultured human cells. Fifty percent inhibition of cholesterol synthesis in human enterocytes was observed at a lovastatin concentration of about 0.004 ng/ml and in other cells at a lovastatin concentration of about 0.03 ng/ml. At lovastatin concentrations between 1.0 and 100.0 ng/ml, a moderate tissue selectivity of lovastatin action was noted. At optimal concentrations, lovastatin inhibited cholesterol synthesis in hepatocytes by 98%, in normal and LDL-receptor negative fibroblasts, arterial smooth muscle cells and hepatoma G-2 cells by about 90%, and in enterocytes by 75%. In rat enterocytes lovastatin inhibited cholesterol synthesis by only 60%.