[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: A Iu Misharin, A S Krylov, C Alquier, H LaFont, A Ia Shteĭnshneĭder, V A Kosykh, A D Morozkin
• Journal: Bioorganicheskaia khimiia (Bioorg Khim) Vol. 23 Issue 4 Pg. 297-303 (Apr 1997) ISSN: 0132-3423 [Print] Russia (Federation)
• Vernacular Title: Srodstvo 3beta-(2-gidroksiétoksi)-5alpha-kholest-8(14)-en-15-ona k oksisterinsviazyvaiushchemu belku i ego metabolizm v kletkakh gepatomy HepG2.
• PMID: 9221731 (Publication Type: English Abstract, Journal Article)

Chemical References

• Hydroxymethylglutaryl-CoA Reductase Inhibitors
• Receptors, Steroid
• oxysterol binding protein
• cholest-8(14)-ene-3,26-diol-15-one
• Cholesterol

Topics

• Animals
• Carcinoma, Hepatocellular (enzymology, metabolism, pathology)
• Cholesterol (analogs & derivatives, metabolism)
• Humans
• Hydroxymethylglutaryl-CoA Reductase Inhibitors
• Liver Neoplasms (enzymology, metabolism, pathology)
• Rabbits
• Receptors, Steroid (metabolism)
• Tumor Cells, Cultured