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%.
Sviridov
D D
DD
Institute of Experimental Cardiology, USSR Cardiology Research Center, Moscow, USSR.
Safonova
I G
IG
Pavlov
M Y
MY
Kosykh
V A
VA
Podrez
E A
EA
Antonov
A S
AS
Fuki
I V
IV
Repin
V S
VS
D000924:Anticholesteremic Agents; D006528:Carcinoma, Hepatocellular / Q000378:metabolism; D002478:Cells, Cultured; D002784:Cholesterol / Q000096:biosynthesis*; D004305:Dose-Response Relationship, Drug; D005347:Fibroblasts / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism; D007422:Intestines / Q000187:drug effects; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D008113:Liver Neoplasms / Q000378:metabolism; D008148:Lovastatin / Q000494:pharmacology*; D009131:Muscle, Smooth, Vascular / Q000378:metabolism; D011973:Receptors, LDL / Q000378:metabolism; D014407:Tumor Cells, Cultured
D000924:Anticholesteremic Agents; D011973:Receptors, LDL; D002784:Cholesterol; D008148:Lovastatin