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

Piir E.A.1, Medvedeva N.V.1, Kashirina N.M.2, Shevelev A.Ya.2, Misharin A.Yu.1

1. V.N. Orechovisch Institute of Biomedical Chemistry, RAMS
2. Institute of Experimental Cardiology, Cardiology Research Center.
Section: Experimental/Clinical Study
PubMed Id: 15628598
Year: 2004  Volume: 50  Issue: 5  Pages: 484-492
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.
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Piir E.A., Medvedeva N.V., Kashirina N.M., Shevelev A.Ya., Misharin A.Yu. (2004) Biomeditsinskaya khimiya, 50(5), 484-492.
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