目的 評(píng)價(jià)注射用益氣復(fù)脈（凍干，YQFM）對(duì)人原代肝細(xì)胞中的藥物代謝酶CYP1A2、2B6和3A4是否具有誘導(dǎo)作用。方法 采用3個(gè)單供體的人原代肝細(xì)胞分別與不同質(zhì)量濃度（0.026、0.260和2.600 mg/mL）的YQFM或特異性誘導(dǎo)劑（CYP1A2誘導(dǎo)劑：50 μmol/L奧美拉唑；CYP2B6誘導(dǎo)劑：1 000 μmol/L苯巴比妥；CYP3A4誘導(dǎo)劑：25 μmol/L利福平）于37℃、5% CO₂條件下共孵育3 d，液質(zhì)聯(lián)用技術(shù)（LC-MS/MS）檢測(cè)酶活性，實(shí)時(shí)熒光定量PCR技術(shù)檢測(cè)CYP1A2、2B6和3A4 mRNA表達(dá)量。結(jié)果 YQFM在測(cè)試濃度條件下對(duì)人原代肝細(xì)胞的CYP1A2、CYP2B6和CYP3A4的酶活性和mRNA的表達(dá)均無(wú)誘導(dǎo)作用。結(jié)論 YQFM不具有顯著的基于藥物代謝酶誘導(dǎo)的中藥和化學(xué)藥的相互作用。

Objective To evaluate the effect of Yiqi Fumai Lyophilized Injection (YQFM) on the drug metabolism enzyme CYP1A2, 2B6 and 3A4 in human primary hepatocytes. Methods In this study, human primary hepatocytes were used from three individual donor, and incubated with different concentrations (0.026, 0.260 and 2.600 mg/mL) of YQFM or specific inducer (CYP1A2 inducer:50 μmol/L Omeprazole; CYP2B6 inducer:1 000 μmol/L Phenobarbital; CYP3A4 inducer:25 μmol/L Rifampicin) under condition of 37℃ and 5% CO₂ for 3 d. The enzyme activity was determined by liquid chromatography-mass spectrometry (LC-MS/MS), and mRNA expression of CYP1A2, 2B6 and 3A4 was detected by fluorescent quantitative PCR. Results:YQFM showed no induction on CYP1A2, CYP2B6 and CYP3A4 enzyme activities and mRNA expression in human primary hepatocytes under test concentration. Conclusion YQFM does not have a significant Herb-Drug Interaction (HDI) based on the induction of drug metabolism enzyme.