机构：[1]School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China[2]Second Affiliated Hospital, Guangzhou University of Chinese Medicine, Guangzhou, China广东省中医院
1. In this article, the modulatory effects of extracts from vinegar-baked Radix Bupleuri (VBRB) and saikosaponins on the activity of CYP1A2, CYP2C9 and CYP3A4 were investigated in vitro. 2. Microsomal in vitro incubation method was utilized to simulate metabolic reaction under physiological environment by incubating the marker with liver microsomes in the absence or presence of VBRB and saikosaponins. The contents of 4-acetamidophenol, 6 beta-hydroxyltestosterone and 4-hydroxydiclofenac, the metabolites of phenacetin, testosterone and diclofenac, which were selected as specific probe drugs of CYP1A2, CYP2C9 and CYP3A4, respectively, were analyzed by high-performance liquid chromatography. 3. The production of the metabolites was incubation time dependent. The modulatory effects of different VBRB extracts and saikosaponins on CYP isoforms increased with concentration. Among all the extracts studied, BC1 has a strong inhibition effect compared to the three CYP isoforms tested, while the others have only significant inhibition on the activity of CYP2C9. 4. This in vitro study demonstrated that various extracts of VBRB tested in this study have negligible potential to interfere with CYP1A2- and CYP3A4-metabolized drugs; risk of herb-drug interaction might occur when VBRB is concurrently taken with CYP2C9 substrates.
基金：
This research was financially supported by the National
Natural Science Foundation of China (grant no. 30672668,
81073063).
第一作者机构：[1]School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China
通讯作者：
通讯机构：[1]School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China[2]Second Affiliated Hospital, Guangzhou University of Chinese Medicine, Guangzhou, China[*1]School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, 110016 Shenyang, China.[*2]Second Affiliated Hospital, Guangzhou University of Chinese Medicine, Neihuan Xilu, Guangzhou Daxuecheng, 510006, Guangzhou, China.
推荐引用方式(GB/T 7714)：
Tongya Yu,Xianzhi Chen,Yinjie Wang,et al.Modulatory effects of extracts of vinegar-baked Radix Bupleuri and saikosaponins on the activity of cytochrome P450 enzymes in vitro[J].XENOBIOTICA.2014,44(10):861-867.doi:10.3109/00498254.2014.914600.
APA：
Tongya Yu,Xianzhi Chen,Yinjie Wang,Ruizhi Zhao&Shirui Mao.(2014).Modulatory effects of extracts of vinegar-baked Radix Bupleuri and saikosaponins on the activity of cytochrome P450 enzymes in vitro.XENOBIOTICA,44,(10)
MLA：
Tongya Yu,et al."Modulatory effects of extracts of vinegar-baked Radix Bupleuri and saikosaponins on the activity of cytochrome P450 enzymes in vitro".XENOBIOTICA 44..10(2014):861-867
