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Methods and Findings
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Methods Find Exp Clin Pharmacol 2010, 32(3): 163
ISSN 0379-0355
Copyright 2010 Clarivate Analytics
CCC: 0379-0355
DOI: 10.1358/mf.2010.32.3.1434161
 
 
Inhibitory effects of schisandrin A and schisandrin B on CYP3A activity
Li, W.L., Xin, H.W., Su, M.W., Xiong, L.
 
 
Our aim was to investigate the inhibitory effects of schisandrin A and schisandrin B on 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 µM and Ki values of 5.83 and 4.24 µM, 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: KI = 4.51 µM, Kinact = 0.134/min; schisandrin B: KI = 3.01 µM, Kinact = 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.


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