丁香酚对人肝微粒体中细胞色素P450 1A2、2C9、2D6和3A4活性的影响。
Effect of eugenol on cytochrome P450 1A2, 2C9, 2D6, and 3A4 activity in human liver microsomes.
作者信息
Alharbi Naif Fahad M, Ahad Abdul, Bin Jardan Yousef A, Al-Jenoobi Fahad I
机构信息
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
出版信息
Saudi Pharm J. 2024 Jul;32(7):102118. doi: 10.1016/j.jsps.2024.102118. Epub 2024 May 23.
This study aimed to provide an understanding of the influence of eugenol on CYP1A2, 2C9, 2D6, and 3A4 in human liver microsomes (HLM). Specific substrate for CYP1A2, 2C9, 2D6, and 3A4 were incubated in HLM with or without eugenol. The formation of their respective metabolites was assessed with HPLC analytical methods. Eugenol at 1, 10 and 100 µM levels inhibited the activity of CYP1A2 and CYP2C9 by 23.38 %, 23.57 %, 39.80 % and 62.82 %, 63.27 %, 67.70 % respectively. While, CYP2D6 and CYP3A4 activity was decreased by 40.70 %, 45.88 %, 62.68 % and 37.41 %, 42.58 % and 67.86 % at 1, 10 and 100 µM eugenol level respectively. The IC value of eugenol for CYP2D6 and CYP3A4 was calculated as 11.09 ± 3.49 µM and 13.48 ± 3.86 µM respectively. Potential herb-drug interactions was noted when eugenol is administered simultaneously with medications metabolized by these enzymes, most notably CYP2C9, CYP2D6 and CYP3A4.
本研究旨在了解丁香酚对人肝微粒体（HLM）中CYP1A2、2C9、2D6和3A4的影响。将CYP1A2、2C9、2D6和3A4的特异性底物在有或没有丁香酚的情况下于HLM中孵育。用HPLC分析方法评估它们各自代谢物的形成。1、10和100µM水平的丁香酚分别使CYP1A2和CYP2C9的活性抑制23.38%、23.57%、39.80%以及62.82%、63.27%、67.70%。而在1、10和100µM丁香酚水平时，CYP2D6和CYP3A4的活性分别降低40.70%、45.88%、62.68%以及37.41%、42.58%、67.86%。丁香酚对CYP2D6和CYP3A4的IC值分别计算为11.09±3.49µM和13.48±3.86µM。当丁香酚与由这些酶代谢的药物同时给药时，注意到存在潜在的药草-药物相互作用，最显著的是CYP2C9、CYP2D6和CYP3A4。
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