对人肝微粒体中紫檀芪对 CYP1A2、CYP2C9 和 CYP2D6 的抑制作用。
The inhibition of CYP1A2, CYP2C9, and CYP2D6 by pterostilbene in human liver microsomes.
机构信息
Department of Clinical Pharmacy 1 , College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj.
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh.
出版信息
Pharmazie. 2021 Apr 1;76(4):155-158. doi: 10.1691/ph.2021.1304.
This study used human liver microsomes to assess pterostilbene's effect on the metabolic activity of cytochrome P450 (CYP) 1A2, CYP2C9, and CYP2D6. The metabolism of their substrates (phenacetin, tolbutamide, and dextromethorphan) was assayed by quantifying their relevant metabolites by HPLC. The IC value was used to express the strength of inhibition, and the value of a volume per dose index (VDI) was used to indicate the metabolic ability of the enzyme. In this study, pterostilbene inhibited CYP1A2, CYP2C9, and CYP2D6's metabolic activities . CYP2C9's activity was most significantly inhibited by pterostilbene; its IC50 value was 0.12±0.04 μM. The IC50 value of CYP1A2 and CYP2D6 was 56.3±10.4 μM and 62.33±11.4 μM, respectively. The finding that suggests that pterostilbene has the potential to interact with CYP2C9 substrates . These results warrant clinical studies to assess the significance of these interactions.
本研究使用人肝微粒体评估了紫檀芪对细胞色素 P450（CYP）1A2、CYP2C9 和 CYP2D6 代谢活性的影响。通过 HPLC 定量分析其底物（非那西汀、甲苯磺丁脲和右美沙芬）的相关代谢物来测定其代谢。IC 值用于表示抑制强度，体积剂量指数（VDI）的值用于表示酶的代谢能力。在这项研究中，紫檀芪抑制了 CYP1A2、CYP2C9 和 CYP2D6 的代谢活性。紫檀芪对 CYP2C9 的活性抑制最为显著；其 IC50 值为 0.12±0.04 μM。CYP1A2 和 CYP2D6 的 IC50 值分别为 56.3±10.4 μM 和 62.33±11.4 μM。这一发现表明紫檀芪有可能与 CYP2C9 底物发生相互作用。这些结果需要进行临床研究以评估这些相互作用的意义。
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