title: [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].
abstract: 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.
authors.forename: A Iu
authors.initials: AIu
authors.lastname: Misharin
authors.forename: A S
authors.initials: AS
authors.lastname: Krylov
authors.forename: C
authors.initials: C
authors.lastname: Alquier
authors.forename: H
authors.initials: H
authors.lastname: LaFont
authors.forename: A Ia
authors.initials: AIa
authors.lastname: Shteĭnshneĭder
authors.forename: V A
authors.initials: VA
authors.lastname: Kosykh
authors.forename: A D
authors.initials: AD
authors.lastname: Morozkin
mesh_terms: 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
chemical_list: D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D011987:Receptors, Steroid; D000098825:Oxysterol Binding Proteins; C055090:cholest-8(14)-ene-3,26-diol-15-one; D002784:Cholesterol