目的:研究苦参碱(Matrine)对CYP3A4转录激活、mRNA诱导作用的影响,并对其在联合用药中药物的相互作用进行评价。方法:利用CCK-8方法检测苦参碱对人结直肠癌LS174T细胞、人肝癌Hep G2细胞增殖的影响;瞬时共转染报告基因方法检测苦参碱对人孕烷X受体(PXR)介导的CYP3A4荧光素酶活性影响;Real-time PCR检测苦参碱对人孕烷X受体、CYP3A4 mRNA诱导作用影响。结果:在一定的浓度范围内,苦参碱对Hep G2和LS174T细胞的增殖均具有抑制作用;在Hep G2细胞中,苦参碱可通过激活PXR而诱导CYP3A4转录,并通过诱导PXR mRNA表达进而上调CYP3A4 mRNA表达。在LS174T细胞中,苦参碱可通过激活PXR诱导CYP3A4转录,并通过诱导PXR mRNA表达进而上调CYP3A4 mRNA表达,且其作用呈浓度依赖性。结论:苦参碱对CYP3A4的诱导可能与人孕烷X受体通路有关,与其他药物联合使用时有可能干扰其他药物的代谢。 OBJECTIVE: To study the effect of matrine on CYP3A4 transcriptional activation and mRNA induction, and to evaluate its interaction with drugs in combination therapy. Methods: The effects of matrine on the proliferation of human colorectal cancer LS174T cells and human hepatocellular carcinoma Hep G2 cells were detected by CCK-8 assay. The effects of matrine on human pregnane X receptor (PXR) The effect of matrine on the induction of human pregnane X receptor and CYP3A4 mRNA was examined by Real-time PCR. Results: Matrine inhibited the proliferation of Hep G2 and LS174T cells in a certain concentration range. In Hep G2 cells, matrine induced the transcription of CYP3A4 by activating PXR, and by inducing PXR mRNA expression Upregulate CYP3A4 mRNA expression. In LS174T cells, matrine can induce CYP3A4 transcription by activating PXR, and up-regulate CYP3A4 mRNA expression by inducing PXR mRNA expression in a concentration-dependent manner. CONCLUSION: The induction of CYP3A4 by matrine may be related to human pregnane X receptor pathway. When combined with other drugs, it may interfere with the metabolism of other drugs.