Effect of eugenol on cytochrome P450 1A2, 2C9, 2D6, and 3A4 activity in human liver microsomes

IF 3 3区医学 Q2 PHARMACOLOGY & PHARMACY

Saudi Pharmaceutical Journal Pub Date : 2024-05-23 DOI:10.1016/j.jsps.2024.102118

Naif Fahad M. Alharbi, Abdul Ahad, Yousef A. Bin Jardan, Fahad I. Al-Jenoobi

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引用次数: 0

Abstract

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 IC₅₀ 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.

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丁香酚对人肝脏微粒体中细胞色素 P450 1A2、2C9、2D6 和 3A4 活性的影响

本研究旨在了解丁香酚对人肝脏微粒体（HLM）中 CYP1A2、2C9、2D6 和 3A4 的影响。将 CYP1A2、2C9、2D6 和 3A4 的特定底物与丁香酚或不与丁香酚一起在 HLM 中培养。采用 HPLC 分析方法评估其各自代谢物的形成。丁香酚在 1、10 和 100 µM 水平下分别抑制 CYP1A2 和 CYP2C9 的活性 23.38 %、23.57 %、39.80 % 和 62.82 %、63.27 %、67.70 %。而在 1、10 和 100 µM 丁香酚水平下，CYP2D6 和 CYP3A4 活性分别降低了 40.70 %、45.88 %、62.68 % 和 37.41 %、42.58 % 和 67.86 %。经计算，丁香酚对 CYP2D6 和 CYP3A4 的 IC50 值分别为 11.09 ± 3.49 µM 和 13.48 ± 3.86 µM。当丁香酚与由这些酶代谢的药物（尤其是 CYP2C9、CYP2D6 和 CYP3A4）同时服用时，可能会发生草药与药物之间的相互作用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Saudi Pharmaceutical Journal PHARMACOLOGY & PHARMACY-

CiteScore

6.10

自引率

2.40%

发文量

194

审稿时长

67 days

期刊介绍： The Saudi Pharmaceutical Journal (SPJ) is the official journal of the Saudi Pharmaceutical Society (SPS) publishing high quality clinically oriented submissions which encompass the various disciplines of pharmaceutical sciences and related subjects. SPJ publishes 8 issues per year by the Saudi Pharmaceutical Society, with the cooperation of the College of Pharmacy, King Saud University.