Gibbons G F, Pullinger C R
Biochem J. 1977 Feb 15;162(2):321-30. doi: 10.1042/bj1620321.
Triparanol [2-(4-chlorophenyl)-1-(4-diethylaminoethoxyphenyl)-1-p-tolylethanol] at a concentration of 2 micronm has no effect on the overall conversion of [2=14C]acetate into C27 sterols by isolated liver cells. In the presence of triparanol, however, the formation of radioactive cholesterol is inhibited by 85-90% and the balance of radioactivity appears in the C27 sterol desmosterol (cholesta-5,24-dien-3beta-ol). The very small weights of desmosterol which accumulate under these conditions were, as a routine, quantitatively converted into the heptafluorobutyrate 3-enol ester of cholesta-4,24-dien-3-one. This derivative has a high electron-capturing capability, a property that enables extremely small quantities (less than 0.25pmol) of the material to be accurately measured by gas chromatography with electron-capture detection. Measurements of the mass and specific radioactivity of the newly biosynthesized desmosterol formed in the presence of triparanol provides an accurate assessment of the amount of cholesterol that would be synthesized by the liver cells in the absence of the drug.
曲帕拉醇[2-(4-氯苯基)-1-(4-二乙氨基乙氧基苯基)-1-对甲苯基乙醇]浓度为2微摩尔时，对分离的肝细胞将[2-¹⁴C]乙酸转化为C27甾醇的总体转化率没有影响。然而，在曲帕拉醇存在的情况下，放射性胆固醇的形成受到85%-90%的抑制，放射性平衡出现在C27甾醇胆甾烯醇（胆甾-5,24-二烯-3β-醇）中。在这些条件下积累的极少量胆甾烯醇，通常会定量转化为胆甾-4,24-二烯-3-酮的七氟丁酸3-烯醇酯。该衍生物具有高电子捕获能力，这一特性使得极少量（小于0.25皮摩尔）的物质能够通过带有电子捕获检测的气相色谱法进行精确测量。对在曲帕拉醇存在下新生物合成的胆甾烯醇的质量和比放射性进行测量，可以准确评估在无该药物情况下肝细胞合成的胆固醇量。
