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3-β-(ω-羟基烷氧基)胆甾-5-烯对兔肝细胞胆固醇生物合成的抑制作用

[Inhibition of cholesterol biosynthesis in rabbit hepatocytes by 3-beta-(omega-hydroxyalkoxy)cholest-5-enes].

作者信息

Maliugin A V, Novikov D K, Kosykh V A, Kosenkov E I, Medvedeva N V, Valentinova N V, Shteĭnshneĭder A Ia, Misharin A Iu

出版信息

Bioorg Khim. 1996 Jul;22(7):541-7.

PMID:8992960
Abstract

3 beta-(2-Hydroxyethoxy)-, 3 beta-(4'-hydroxybutoxy)-, 3 beta-(6-hydroxyhexyloxy)-, 3 beta-(9-hydroxynonyloxy)-, and 3 beta-(2-hydroxy-2-[3H]ethoxy)cholest-5-enes were synthesized. By means of a spin probe, the influence of the synthesized compounds on the phase transition of dimyristoylphosphatidylcholine were estimated. Time and dose dependences of the incorporation of 3 beta-(2-hydroxy-2-[3H]ethoxy)cholest-5-ene into rabbit hepatocytes (the primary culture) were studied. 3 beta-(2-Hydroxyethoxy)- and 3 beta-(4-hydroxybutoxy)cholest-5-enes were shown to inhibit cholesterol biosynthesis from [14C]acetate in rabbit hepatocyte cultures upon a 24-hour preincubation.

摘要

合成了3β-(2-羟基乙氧基)-、3β-(4'-羟基丁氧基)-、3β-(6-羟基己氧基)-、3β-(9-羟基壬氧基)-和3β-(2-羟基-2-[3H]乙氧基)胆甾-5-烯。借助自旋探针,评估了合成化合物对二肉豆蔻酰磷脂酰胆碱相变的影响。研究了3β-(2-羟基-2-[3H]乙氧基)胆甾-5-烯掺入兔肝细胞(原代培养)的时间和剂量依赖性。经24小时预孵育后,3β-(2-羟基乙氧基)-和3β-(4-羟基丁氧基)胆甾-5-烯显示出抑制兔肝细胞培养物中由[14C]乙酸盐合成胆固醇的作用。

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