Effects of (22s,23s)- and (22r,23r)-3β-hydroxy-22,23-oxido-5α-ergost-8(14)-en-15-ones on cholesteryl esters biosynthesis and acyl-coa:cholesterol acyl transferase activity in hep g2 cells

   


1. Orekhovich Institute of Biomedical Chemistry, RAMS
Type: Experimental/clinical study
UDK: 547.92.057      PubMed Id: 18712089
Year: 2008 vol: 54  issue:3  pages: 341-348
Abstract: Novel synthetic oxysterols (22S,23S)-3β-hydroxy-22,23-oxido-5α-ergost-8(14)-en-15-one (I) and (22R,23R)-3β-hydroxy-22,23-oxido-5α-ergost-8(14)-en-15-one (II) influenced cholesteryl esters biosynthesis in human hepatoma Hep G2 cell line from [14C]acetate (85% and 180% compared to control at the concentrations of 5 μМ). The level of cholesteryl esters biosynthesis in Hep G2 cells from [14C]oleate increased in the presence of ketosterol (I) in a dose dependent manner, whereas the level of cholesteryl esters biosynthesis in the presence of ketosterol (II) reached the maximal value (269±20% from control) at the concentration of 1 µM. In a cell free system ketosterol (I) increased the rate of ACAТ-dependent cholesterol acylation like 25-hydroxycholesterol, however, ketosterol (II), efficiently stimulating initial rate of АСАТ-catalyzed cholesterol esterification, caused in rapid inactivation of this enzyme.
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Reference: Mehtiev A.R., Kozlova N.I., Skripnik V.V., Misharin A.Yu., Effects of (22s,23s)- and (22r,23r)-3β-hydroxy-22,23-oxido-5α-ergost-8(14)-en-15-ones on cholesteryl esters biosynthesis and acyl-coa:cholesterol acyl transferase activity in hep g2 cells, Biomeditsinskaya khimiya, 2008, vol: 54(3), 341-348.
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