[Affinity of 3-beta-(2-hydroxyethoxy)-5-alpha-cholest-8(14)-ene-15-one to oxysterol binding protein and its metabolism in HepG2 hepatoma cells].
beta-(2-Hydroxyethoxy)-5 alpha-cholest-8(14)-en-15-one, a synthetic inhibitor of cholesterol biosynthesis, was shown to exhibit a high affinity to oxysterol binding protein. This was proved by ultracentrifugation of the protein fraction from rabbit liver in the presence of the 3H-labeled inhibitor, 3 beta-(2-hydroxy-2-[3H]ethoxy)-5 alpha-cholest-8(14)-en-15-one, or by the substitution of the [3H]-25-hydroxycholesterol in its complex with the oxysterol binding protein. In human hepatoma Hep G2 cells, the inhibitor decreased activity of 3-hydroxy-3-methylglutaryl CoA reductase [ID50 (2.7 +/- 0.7) x 10(-5) M] and was transformed into 3 beta-[2-(9-Z-octadecenoyloxy)ethoxy]-5 alpha-cholest-8(14)-en-15-one.
Misharin
A Iu
AIu
Krylov
A S
AS
Alquier
C
C
LaFont
H
H
Shteĭnshneĭder
A Ia
AIa
Kosykh
V A
VA
Morozkin
A D
AD
D000818:Animals; D006528:Carcinoma, Hepatocellular / Q000201:enzymology / Q000378:metabolism* / Q000473:pathology; D002784:Cholesterol / Q000031:analogs & derivatives* / Q000378:metabolism; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D008113:Liver Neoplasms / Q000201:enzymology / Q000378:metabolism* / Q000473:pathology; D011817:Rabbits; D011987:Receptors, Steroid / Q000378:metabolism*; D014407:Tumor Cells, Cultured; D000098825:Oxysterol Binding Proteins
D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D011987:Receptors, Steroid; D000098825:Oxysterol Binding Proteins; C055090:cholest-8(14)-ene-3,26-diol-15-one; D002784:Cholesterol