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目的为了评价含厚朴酚的中药干预异丙酚在人体内代谢的风险。方法在人肠、肝、肾微粒体体系中,通过动力学分析的方法,在体外探讨了厚朴酚对各微粒体催化异丙酚葡萄糖醛酸转移代谢活性的抑制能力。结果厚朴酚能显著抑制异丙酚在人肝、肾微粒体中的葡萄糖醛酸结合代谢反应,抑制过程均遵循混合抑制动力学模型,抑制常数Ki分别为0.1和0.2μmol·L~(-1)。与人肝、肾微粒体不同,人肠微粒体中异丙酚的葡萄糖醛酸结合代谢不受厚朴酚的影响。结论含厚朴酚的中药,在人整体水平上难以抑制异丙酚葡萄糖醛酸结合代谢路径。
Objective To evaluate the effect of honokiol-containing Chinese medicine on the risk of propofol metabolism in the human body. Methods The inhibitory effect of magnolol on the catalytic activity of propofol glucuronide metabolism in vitro was investigated by kinetic analysis in human intestinal, hepatic and renal microsomes. Results Honokiol could significantly inhibit the glucuronide-binding metabolic reaction of propofol in human liver and kidney microsomes. The inhibition process followed the mixed inhibition kinetic model with inhibition constants Ki of 0.1 and 0.2 μmol·L ~ (-1) 1). Unlike human liver and kidney microsomes, the glucuronide-binding metabolism of propofol in human intestinal microsomes is not affected by honokiol. Conclusions Chinese herbal medicine containing magnolol can not inhibit propofol-glucuronide-binding metabolic pathway on the whole human body.