目的 研究白芷香豆素类化合物（欧前胡素、异欧前胡素、佛手柑内酯、氧化前胡素）在体外对P-糖蛋白（P-gp）三磷酸腺苷（ATP）酶活性的影响，进而探讨白芷香豆素类成分影响P-gp介导药物转运的机制。方法 采用ATP酶活性测试法判断白芷香豆素类化合物是否为P-gp的底物。结果 欧前胡素和氧化前胡素各质量浓度组平均荧光强度值（ΔRLU_TC）均大于基础平均荧光强度值（ΔRLU_basal）；异欧前胡素中、低质量浓度组及佛手柑内酯高、低质量浓度组ΔRLU_TC小于ΔRLU_basal。结论 欧前胡素和氧化前胡素为非浓度依赖的P-gp ATP酶抑制剂，异欧前胡素、佛手柑内酯在低质量浓度时可抑制ATP酶活性，对P-gp具有抑制作用；在高质量浓度时可诱导ATP酶活性，对P-gp具有诱导作用。

Objective To study the effects of coumarins in Angelicae Dahuricae Radix (imperatorin, isoimperatorin, bergapten, and oxypeucedanin) on the activities of adenosine triphosphate (ATPase) in P-glycoprotein (P-gp) in vitro and to investigate the P-gp mediated meschanism in transport of drug. Methods The ATPase activity assay was used to identify whether the coumarins in Angelicae Dahuricae Radix were P-gp substrates or not. Results The average fluorescent values (ΔRLU_TC) of imperation and oxypeucedanin at each concentration were greater than average basic fluorescence value (ΔRLU_basal). The average fluorescent values (ΔRLU_TC) in medium and low concentration of isoimperatorin and bergapten groups were lower than average basic fluorescence value (ΔRLU_basal). Conclusion Imperation and oxypeucedanun are non-concentration dependent P-gp ATP inhibitors. Isoimperatorin and bergamot lactones could inhibit the ATPase activity at low concentration and have the inhibitory effect on P-gp. At high concentration, the activity of ATPase can be induced so as to induce P-gp.

江西省青年科学基金资助项目（20161ACB21020）；江西省青年科学家培养对象资助项目（20153BCB23019）；国家青年自然科学基金资助项目（81303237）；中国博士后基金（2016M590606）