- 生物活性
7α-Hydroxy-4-cholesten-3-one 是一种由胆固醇合成胆汁酸的中间体。7α-Hydroxy-4-cholesten-3-one 是一种孕烷 X 受体 (PXR) 激动剂。7α-Hydroxy-4-cholesten-3-one 是胆汁酸流失，肠易激综合征和其他与胆汁酸生物合成缺陷有关的疾病的生物标志物。7α-Hydroxy-cholest-4-en-3-one 也是一种 CYP8B1 的生理底物。
- 靶点
Endogenous Metabolite
Pregnane X receptor (PXR)
- 体外研究
7α-Hydroxy-4-cholesten-3-one is found relatively upstream in the biosynthetic pathway to bile acids (e.g. chenodeoxycholic acid). The first step is the incorporation of the 7α-hydroxy group onto cholesterol by cytochrome P450 7A1, and the second step is the oxidation and isomerization of the 3-hydroxy group and the Δ5,6-double bond by 3β-hydroxy steroid dehydrogenase to yield 7α-Hydroxy-4-cholesten-3-one. The deletion of the gene that expresses P450 27A1, which is found downstream in the bile acid pathway, results in the accumulation of the precursor, 7α-Hydroxy-4-cholesten-3-one.
- 体内研究
7α-Hydroxy-4-cholesten-3-one strongly relates to the hepatic enzymatic activity of CYP7A1 at steady-state conditions as well as during the rapid diurnal changes that occur in the rat. That serum 7α-Hydroxy-4-cholesten-3-one has a pronounced diurnal rhythm.
医药
合成步骤: 1. 胆固醇经CYP7A1催化，引入7α-羟基；2. 经3β-羟基类固醇脱氢酶催化，发生氧化和Δ5,6-双键异构化反应，生成7-羟基-4-胆甾烯-3-酮。相关条件: 涉及CYP7A1和3β-羟基类固醇脱氢酶的酶促反应。特殊情况: P450 27A1基因缺失会导致该物质积累。
