INHIBITORY EFFECTS OF SCHISANDRIN A AND SCHISANDRIN B ON CYP3A ACTIVITY

被引：25
|
作者：
Li, W. L. [1 ]
Xin, H. W. [1 ]
Su, M. W. [1 ]
Xiong, L. [1 ]
机构：
[1] Wuhan Gen Hosp Guangzhou Command, Dept Clin Pharmacol, Wuhan 430070, Peoples R China
来源：
METHODS AND FINDINGS IN EXPERIMENTAL AND CLINICAL PHARMACOLOGY | 2010年 / 32卷 / 03期
关键词：
IN-VITRO; P-GLYCOPROTEIN; SPHENANTHERA EXTRACT; MULTIDRUG-RESISTANCE; LIVER-MICROSOMES; ORGANIC-SOLVENTS; MIDAZOLAM; DRUGS; PHARMACOKINETICS; METABOLISM;
D O I：
10.1358/mf.2010.32.3.1434161
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Our aim was to investigate the inhibitory effects of schisandrin A and schisandrin Ban cytochrome P450 (CYP3A) activity in rat liver microsomes and the mechanism of this interaction. 1'-Hydroxy midazolam and midazolam 1-hydroxylation catalyzed by CYP3A were analyzed by high performance liquid chromatography (HPLC). Results showed that schisandrin A and schisandrin B inhibited CYP3A activity with IC50 values of 6.60 and 5.51 mu M and K-i Values of 5.83 and 4.24 mu M, respectively. A dilution assay plot of each inhibitor gave a slope value of up to 91% that of the control samples. The inactivation of CYP3A activity by schisandrin A and schisandrin B was found to be both time- and concentration-dependent (schisandrin A: K-i = 4.51 mu M, K-inact = 0.134/min; schisandrin B: K-i = 3.01 mu M, K-inact = 0.112/min). We conclude that the inhibition of CYP3A activity in rat liver microsomes by schisandrin A and schisandrin B is mostly attributed to a mixed noncompetitive and complete inhibition.
引用
收藏
页码：163 / 169
页数：7
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