Interaction of acyl derivatives of 3β-hydroxy-5α-cholest-8(14)-en-15-one and 3α-hydroxy-5a-cholest-8(14)-en-15-one with hepatoma Hep G2 cells

   


1. V.N. Orechovisch Institute of Biomedical Chemistry, RAMS
2. Institute of Experimental Cardiology, Cardiology Research Center.
Type: Experimental/clinical study
PubMed Id: 15628598
Year: 2004 vol: 50  issue:5  pages: 484-492
Abstract: Effects of 3β-hydroxy-5α-cholest-8(14)-en-15-one (I), 3α-hydroxy-5α-cholest-8(14)-en-15-one (II), 3β-hexadecanoyloxy-5α-cholest-8(14)-en-15-one (III), 3α-hehadecanoyloxy-5a-cholest-8(14)-en-15-one (IV), 3β-acetoxy-5α-cholest-8(14)-en-15-one (V), 3α-acetoxy-5α-cholest-8(14)-en-15-one (VI) on cholesterol metabolism in hepatoma Hep G2 cells were studied. Compound III slowly bind to Hep G2 cells followed by internalization and metabolic transformation (at a concentration of 30 µM the total binding of compound III was (3.9±0.4) nmol per 1 mg of cell protein for 24 h incubation). Compound I depressed and compound III stimulated the uptake of low density lipoproteins radiolabeled with oleyl cholesteryl ether [14C-CE]LDL (58% and 149% from control). Compounds I and II inhibited cholesterol biosynthesis from [14C]аcetate (with IC50 values of 4.0±0.7 and 8.0±1.5 µМ). Effects of compounds V and VI were less potent; compounds III and IV were inactive. Compound II activated cholesterol acylation, estimated by incorporation of [14C]-oleic acid into cholesteryl esters (170% from control at a concentration of 30 µМ). The results indicate correlation between polarity of the compound and its ability to regulate cholesterol metabolism in Hep G2 cells.
Download PDF:
Reference: Piir E.A., Medvedeva N.V., Kashirina N.M., Shevelev A.Ya., Misharin A.Yu., Interaction of acyl derivatives of 3β-hydroxy-5α-cholest-8(14)-en-15-one and 3α-hydroxy-5a-cholest-8(14)-en-15-one with hepatoma Hep G2 cells, Biomeditsinskaya khimiya, 2004, vol: 50(5), 484-492.
Bibliography
 2016(Vol:62)
 2015(Vol:61)
 2014(Vol:60)
 2013(Vol:59)
 2012(Vol:58)
 2011(Vol:57)
 2010(Vol:56)
 2009(Vol:55)
 2008(Vol:54)
 2007(Vol:53)
 2006(Vol:52)
 2005(Vol:51)
 2004(Vol:50)
 2003(Vol:49)