Evaluation of the Effects of Wuweizi and Nan Wuweizi Extract on Human Liver Microsomal CYP3A4 Enzyme Activity by in Vitro Probe Method
LIN Lujie
ZHANG Mingxiao
LI Hua
YANG Bin
Abstract：Objective The aim was to evaluate the effects of Wuweizi and Nan Wuweizi extract on the enzyme activities of human hepatic cytochrome P450 3A4(CYP3A4)by in vitro probe.Methods Microsomal CYP3A4 activity was determined by measuring the amount of 6β-hydroxytestosterone by liquid chromatography-tandem mass spectrometry combined with a drug probe of testosterone.Results The linear range of 6β-hydroxytestosterone was 15.0～960 μg/L and the correlation coefficient was 0.999 9.The relative recovery was 102.1%～105.7%and the value of relative standard deviation was less than 11%.The activity of the CYP3A4 enzyme was inhibited by the alcohol and aqueous extracts of Wuweizi and Nan Wuweizi.The inhibitory abilities of the alcohol and aqueous extracts of Wuweizi were stronger than those of Nan Wuweizi.In addition,the inhibitory degree of alcohol extracts was stronger than that of water extracts.The inhibitory effect of lignans on the activity of CYP3A4 enzyme was in the order:schisantherin A,schizandrin B,schisandrin A,schizandra A.Conclusion The inhibitory effects of Wuweizi and Nan Wuweizi extracts on CYP3A4 enzyme activity were significantly different(P<0.05).Clinically,the phenomenon of their mixed-use occurred occasionally.If they were in combination with the drugs whose metabolism involves CYP3A4 specificity,some adverse consequences would be caused by metabolic interaction.
Keywords：Nan WuweiziWuweiziLignanHepatic microsomeCYP3A4HPLC-MS/MS
Publication Date：2023-12-28
Online Publishing Date：2025-08-15(First online date of this platform, not the publication date of the document)
Pages：5( 2071-2075 )