Pregna-5,17(20)-dien-21-oyl amides affecting sterol and triglyceride biosynthesis in Hep G2 cells |
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| Authors: | Sergey V Stulov Olga V Mankevich Nikita O Dugin Roman A Novikov Vladimir P Timofeev Alexander Yu Misharin |
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| Institution: | 1. Orekhovich Institute of Biomedical Chemistry, RAMS, Moscow, Russia;2. Engelghardt Institute of Molecular Biology, Russian Academy of Sciences, 32, Vavilov Street, Moscow 119991, Russia |
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| Abstract: | Synthesis of series 17(20)Z]- and 17(20)E]-pregna-5,17(20)-dien-21-oyl amides, containing polar substituents in amide moiety, based on rearrangement of 17α-bromo-21-iodo-3β-acetoxypregn-5-en-20-one caused by amines, is presented. The titled compounds were evaluated for their potency to regulate sterol and triglyceride biosynthesis in human hepatoma Hep G2 cells in comparison with 25-hydroxycholesterol. Three 17(20)E]-pregna-5,17(20)-dien-21-oyl amides at a concentrations of 5 μM inhibited sterol biosynthesis and stimulated triglyceride biosynthesis; their regulatory potency was dependent on the structure of amide moiety; the isomeric 17(20)Z]-pregna-5,17(20)-dien-21-oyl amides were inactive. |
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