孕前X受体激活的物种差异由Δ-9-四大麻素,大麻素和大麻素激活
Aik Jiang Lau1, Thomas K H Chang2
1College of Pharmacy, Faculty of Health, Dalhousie University, Canada; Department of Pharmacology, Faculty of Medicine, Dalhousie University, Canada.
Biochemical and biophysical research communications
|January 9, 2026
概括
大麻化合物如THC,CBD和CBN激活了人类的Pregnane X受体 (PXR). 这项研究表明,这些植物性大麻素作为PXR激动剂,影响药物代谢途径.
科学领域:
- 药理学 药理学是指药理学的学科.
- 分子生物学分子生物学
- 生物化学 生物化学
背景情况:
- 大麻植物含有植物性大麻素,如Δ-9-四基大麻 (THC),大麻 (CBD) 和大麻 (CBN).
- 孕妇X受体 (PXR) 是一个调节药物代谢酶的核受体,如CYP3A4.4.
- 以前的研究表明,THC和CBD会影响人类肝细胞中的CYP3A4表达.
研究的目的:
- 调查THC,CBD和CBN是否作为孕妇X受体 (PXR) 的激动剂.
- 确定这些大麻素对人类 (hPXR),大鼠 (rPXR) 和老鼠 (mPXR) PXR激活的度反应影响.
- 探索大麻素与hPXR.的联结域的相互作用.
主要方法:
- 在PXR转移的HepG2细胞中进行了双露西法酶记者基因测试,以测量受体激活.
- 使用THC,CBD和CBN在不同度下进行了度-反应研究.
- 用哺乳动物单杂交和双杂交试验来评估事务激活和协同激活器招募.
主要成果:
- 根据度,THC,CBD和CBN显著激活了hPXR,rPXR和mPXR.
- 这些大麻素激活hPXR的最低有效度 (MEC) 与rPXR和mPXR相比较低.
- 观察到的证据表明,转换和类固醇受体协同激活器-1的招募到hPXR连接体结合域.
结论:
- THC,CBD和CBN作为人类孕妇X受体 (hPXR) 的激动剂.
- 这些植物性大麻素表现出hPXR的优先激活,而不是老鼠和小鼠的PXR.
- 这些发现表明大麻化合物如何与药物代谢酶调节相互作用的潜在机制.
关键词:
大麻二醇 (Cannabidiol) 是一种卡纳比诺尔 (Cannabinol) 是一种大麻醇.孕妇的X受体受体.类固醇受体联合激活剂-1Δ-9-Tetrahydrocannabinol-Tetrahydrocannabinol-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D-9-Tetrahydrocannabinol-D
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