机构：[a]Department of Pediatrics, Weifang Yidu Central Hospital, Weifang, China[b]Qingzhou Dongxia Central Health Center, Weifang, China[c]Department of Pediatrics, Qujing First People’s Hospital at Kunming Medical University, Qujing, China
Ophiopogonin D is a commonly used herb in cardiology and pediatrics for its variuos pharmacological effects. It is necessary to investigate the effect of ophiopogonin D on the activity of cytochrome P450 enzymes (CYP450s) to provide more guidance for the clinical application of ophiopogonin D. Eight isoforms of CYP450s, including CYP1A2, 2A6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4 were incubated with 100 mu M ophiopogonin D in pooled human liver microsomes. The inhibition model and corresponding parameters were also investigated. Ophiopogonin D exerted a significant inhibitory effect on the activity of CYP3A4, 2C9, and 2E1 in a dose-dependent manner with the IC50 values of 8.08, 12.92, and 22.72 mu M, respectively (p < 0.05). The inhibition of CYP3A4 by ophiopogonin D was performed non-competitively and time-dependently with the Ki value of 4.08 mu M and the KI/K-inact value of 5.02/0.050 min(-1)center dot mu M-1. Whereas, ophiopogonin D acts as a competitive inhibitor of CYP2E1 and 2C9 with the Ki value of 6.69 and 11.07 mu M, respectively. The inhibitory effect of ophiopogonin D on the activity of CYP3A4, 2C9, and 2E1 indicated the potential drug-drug interaction between ophiopogonin D and drugs metabolized by these CYP450s, which needs further in vivo investigation and validation.
第一作者机构：[a]Department of Pediatrics, Weifang Yidu Central Hospital, Weifang, China
共同第一作者：
通讯作者：
通讯机构：[c]Department of Pediatrics, Qujing First People’s Hospital at Kunming Medical University, Qujing, China[*1]Department of Pediatrics, Qujing First People’s Hospital at Kunming Medical University, No. 1, Yuanlin Road, Qujing, Yunnan, 655400, China
推荐引用方式(GB/T 7714)：
Xiaofei Ji,Baodong Ding,Xiaoyou Wu,et al.In vitro study on the effect of ophiopogonin D on the activity of cytochrome P450 enzymes[J].XENOBIOTICA.2021,51(3):262-267.doi:10.1080/00498254.2020.1842941.
APA：
Xiaofei Ji,Baodong Ding,Xiaoyou Wu,Fengyi Liu&Fengqi Yang.(2021).In vitro study on the effect of ophiopogonin D on the activity of cytochrome P450 enzymes.XENOBIOTICA,51,(3)
MLA：
Xiaofei Ji,et al."In vitro study on the effect of ophiopogonin D on the activity of cytochrome P450 enzymes".XENOBIOTICA 51..3(2021):262-267
