Schroepfer G J, Pajewski T N, Hylarides M, Kisic A
Biochem Biophys Res Commun. 1987 Aug 14;146(3):1027-32. doi: 10.1016/0006-291x(87)90750-9.
The metabolism of 5 alpha-cholest-8(14)-en-3 beta-ol-15-one (I), a potent inhibitor of cholesterol synthesis with marked hypocholesteremic activity, has been studied in a nonhuman primate. A mixture of [2,4-3H]-I and [4-14C]-cholesterol was administered to a male baboon in the form of a feedball. Blood was samples at 4, 8, 12, 16, and 24 hr. Detailed analyses of the plasma lipids indicated very rapid absorption of I (relative to cholesterol) and metabolism to cholesterol, cholesteryl esters, and esters of I. The labeled cholesterol was characterized by chromatographic techniques and by purification by way of its dibromide derivative. The levels of 3H in plasma associated with I, esters of I, cholesterol, and cholesteryl esters each showed a different time course. By 24 hr after the administration of [2,4-3H]-I, most of the 3H in plasma was associated with cholesterol and cholesteryl esters. The levels of total 3H and 14C in plasma at various times after the administration of the mixture of [2,4-3H]-I and [4-14C]-cholesterol differed markedly with 3H showing a maximum value at 4 hr and 14C showing a maximum value at 24 hr.
5α-胆甾-8(14)-烯-3β-醇-15-酮（I）是一种具有显著降胆固醇活性的强效胆固醇合成抑制剂，对其在一种非人类灵长类动物中的代谢情况进行了研究。将[2,4-³H]-I和[4-¹⁴C]-胆固醇的混合物制成饲料球喂给一只雄性狒狒。在4、8、12、16和24小时采集血样。对血浆脂质的详细分析表明，I（相对于胆固醇）吸收非常迅速，并代谢为胆固醇、胆固醇酯和I的酯类。标记的胆固醇通过色谱技术并通过其二溴化物衍生物进行纯化来表征。与I、I的酯类、胆固醇和胆固醇酯相关的血浆中³H水平各自呈现出不同的时间进程。在给予[2,4-³H]-I后24小时，血浆中的大部分³H与胆固醇和胆固醇酯相关。在给予[2,4-³H]-I和[4-¹⁴C]-胆固醇混合物后的不同时间，血浆中³H和¹⁴C的总量差异显著，³H在4小时达到最大值，¹⁴C在24小时达到最大值。
