[Transformation of 3beta-(2-hydroxyethoxy)-5alpha-cholest-8(14)-en-15-one in a polar metabolite in HepG2 hepatoma cells].
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| Abstract |
Incubation of 3 beta-(2-hydroxy-2[3H]-ethoxy)-5 alpha-cholest-8(14)-en-15-one with Hep G2 cells led to the accumulation of a radioactive polar product in the culture medium, which was identified as 3 beta-(2-hydroxyethoxy)-15-keto-5 alpha-cholest-8(14)-ene-24-oic acid. Its structure was confirmed by a chemical counter synthesis. The labeled ketosterol was rapidly (tau 1/2 = 6 min) and reversibly bound by Hep G2 cells. The intracellular concentration of 15-ketosterol decreased during incubation mainly due to the formation of a polar metabolite, secreted to the medium. The level of cholesterol biosynthesis was 22 +/- 5% of the control value in Hep G2 cells at a 15-ketocholesterol concentration in the medium of 30 microM. However, further incubation for 3 h in the medium without the ketosterol led to restoration of the level of biosynthesis to 85 +/- 11% of the control value. These results suggest that inhibition of the cholesterol biosynthesis by 15-ketocholesterol in Hep G2 cells depends on the intracellular concentration of the inhibitor, which, in turn, is determined by the rate of its conversion into the polar metabolite. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2003, vol. 29, no. 6; see also http://www.maik.ru.
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| Authors | E A Piĭr, D V Ignatov, N V Medvedeva, A Iu Misharin |
| Journal | Bioorganicheskaia khimiia (Bioorg Khim) 2003 Nov-Dec Vol. 29 Issue 6 Pg. 648-54 ISSN: 0132-3423 [Print] Russia (Federation) |
| Vernacular Title | Prevrashchnie 3beta-(2-gidroksiétoksi)5alpha-kholest-8(14)-en-15-ona v poliarnyĭ metabolit v kletkakh gepatomy HepG2. |
| PMID | 14743540 (Publication Type: English Abstract, Journal Article) |
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