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  • Title: [Interaction of acyl derivatives of 3beta-hydroxy-5alpha-cholest-8(14)-en-15-one and 3alpha-hydroxy-5alpha-cholest-8(14)-en-15-one with hepatoma hep G2 cells].
    Author: Piĭr EA, Medvedeva NV, Kashirina NM, Shevelev AIa, Misharin AIu.
    Journal: Biomed Khim; 2004; 50(5):484-92. PubMed ID: 15628598.
    Abstract:
    Effects of 3beta-hydroxy-5alpha-cholest-8(14)-en-15-one (I), 3alpha-hydroxy-5alpha-cholest-8(14)-en-15 one (II), 3beta-hexadecanoyloxy-5alpha-cholest-8(14)-en-15-one (III), 3alpha-hehadeeanoyloxy-5alpha-cholest-8(14)-en-15-one (IV), 3beta-acetoxy-5alpha-cholest-8(14)-en-15-one (V), 3alpha-acetoxy-5alpha-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 microM 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]acetate (with IC50 values of 4.0 +/- 0.7 and 8.0 +/- 1.5 microM). 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 microM). The results indicate correlation between polarity of the compound and its ability to regulate cholesterol metabolism in Hep G2 cells.
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