目的:研究银杏叶提取物及其中2种主要活性物质黄酮和内酯对人体内CYP3A4酶活性的影响。方法:构建了可用于体外高通量检测基于PXR诱导的CYP3A4系统,通过细胞培养实验,化学发光检测仪检测银杏叶不同组分对CYP3A4的激活水平。采用反相高效液相色谱法测定银杏叶不同组分对细胞内尼卡地平代谢的影响。结果:高通量检测系统检测表明,银杏叶提取物对体内的CYP3A4酶表达具有显著的激活作用。进一步研究证实银杏叶提取物的两类主要活性物质黄酮和内酯呈剂量的方式激活CYP3A4的表达。银杏叶内酯明显加速尼卡地平的代谢速率,而银杏叶黄酮则降低细胞内尼卡地平的降解速率。结论:银杏叶提取物及其主要活性成分黄酮和内酯能显著提高CYP3A4的活性,内酯能提高CYP3A4代谢尼卡地平的能力,而黄酮则可能由于药物相互作用的原因,抑制了CYP3A4酶活性,降低其代谢尼卡地平的能力。 OBJECTIVE: To study the effects of Ginkgo biloba extract and two main active substances, flavonoids and lactones, on CYP3A4 activity in human. Methods: The CYP3A4 system was constructed based on PXR induction in vitro. The cell viability of CYP3A4 was detected by chemiluminescence detector. The effects of different components of Ginkgo biloba leaves on the metabolism of nicardipine in cells were determined by RP-HPLC. Results: High-throughput detection system showed that Ginkgo biloba extract had a significant effect on the expression of CYP3A4 in vivo. Further study confirmed that two main active substances of Ginkgo biloba extract flavonoids and lactones in a dose-dependent manner to activate CYP3A4 expression. Ginkgo biloba lactone significantly accelerated the rate of nicardipine metabolism, while ginkgo leaf flavonoids decreased the rate of intracellular nicardipine degradation. Conclusion: Ginkgo biloba extract and its main active ingredients flavonoids and lactones can significantly increase the activity of CYP3A4, lactone can enhance the ability of CYP3A4 metabolism of nicardipine, but flavonoids may inhibit the CYP3A4 enzyme activity due to drug interactions , Reducing its ability to metabolize nicardipine.