果汁及其成分对CYP2C9活动的抑制动力学
Kana Koinuma1, Tokio Morita2, Yoshinori Uekusa3
1Division of Clinical Pharmacy, Graduate School of Pharmaceutical Sciences, Keio University, 1-5-30, Shibakoen Minato-ku, Tokyo 105-8512, Japan.
Journal of pharmaceutical sciences
|September 11, 2025
概括
贾巴拉果汁提取物 (JEx) 和其成分 (HpMF,HxMF) 抑制细胞染色体P450 (CYP) 2C9的活性. 这项研究表明,贾巴拉果汁可能会通过抑制肠道CYP2C9.9的作用来引起食品药物相互作用.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物新陈代谢 药物新陈代谢
- 自然产品 自然产品
背景情况:
- 之前的研究表明,贾巴拉提取物 (JEx) 抑制CYP3A4,但不抑制CYP2C19.
- 确定HPMF和HxMF是CYP3A4.4的关键抑制剂.
研究的目的:
- 研究JEx,HpMF和HxMF对细胞染色体P450 (CYP) 2C9.9的抑制作用.
- 为了确定这些化合物对CYP2C9抑制的动力学.
主要方法:
- 在体外评估时间依赖和时间独立的抑制动力学.
- 使用人类复合CYP2C9和华法林作为基质.
- 对JEx,HpMF和HxMF针对CYP2C9.9的确定IC50值.
主要成果:
- JEx没有表现出CYP2C9.9的时间依赖抑制.
- 杰克斯,hpmf和hxmf证明了对cyp2c9.9的时间独立抑制.
- IC50值为JEx的2.65%,HpmF的16.2微米,HxMF的57.8微米等价.
结论:
- HpMF和HxMF是JEx介导的CYP2C9抑制的主要贡献者.
- 摄入贾巴拉果汁可能会显著降低肠道CYP2C9活性.
- 贾巴拉果汁有可能通过抑制CYP2C9引起食品药物相互作用.
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