中文摘要：

目的研究四物汤及其有效成分对大鼠肝脏P450酶的影响,从药物代谢酶角度为四物汤的配伍规律提供实验依据。方法大鼠口服灌胃四物汤10 g·kg-1·d-1及其有效成分果糖0.334 g·kg-1·d-1,阿魏酸0.002 g·kg-1·d-1,川芎嗪0.011 g·kg-1·d-1,芍药苷0.022 g·kg-1·d-1,连续给药1周后处死,用生理盐水灌流肝脏,制备肝微粒体,采用混合探针与肝微粒体体外孵育法考察四物汤及其有效成分对大鼠肝脏细胞色素P450酶的影响。利用实时定量聚合酶链式反应（Q-PCR）检测四物汤及其有效成分对大鼠肝脏P450 mRNA表达的影响,利用Western blot法检测四物汤及其有效成分对大鼠肝脏CYP2B1蛋白表达的影响。结果肝微粒体孵育结果显示,果糖对CYP1A2、CYP2B6、CYP2C9、CYP2D6酶活性具有抑制作用,阿魏酸对CYP2C9、CYP2B6酶活性具有抑制作用,川芎嗪对CYP1A2、CYP2C9、CYP2B6的酶活性具有抑制作用,芍药苷对CYP2D6、CYP2B6酶活性具有抑制作用。阿魏酸、果糖、芍药苷组对CYP2B1mRNA的表达具有抑制作用,与酶活性水平一致。4种单体成分对CYP2B1蛋白表达具有抑制作用。结论阿魏酸、果糖、芍药苷组在CYP450酶活性、mRNA基因转录水平及蛋白表达水平对CYP2B1均有抑制作用。

英文摘要：

Aim To study the influence of Si-Wu Decoction（ SWD） and its active components on cytochrome P450 activity and mRNA expression in rats in order to provide an experimental basis for compatibility of SWD. Methods SWD and its active components were intragastrically administrated for seven days,the doses of SWD was 10 g · kg- 1· d- 1,the doses of fructose,ferulic acid, ligustrazine, peoniflorin were0. 334,0. 002,0. 011 and 0. 022 g·kg- 1·d- 1,respectively. After administration for seven days,rats were executed,and liver microsomes were prepared.The effects of SWD and its active components on cytochrome P450 in rats were investigated by hybrid probe and liver microsomes incubation method. The level of mRNA expression in liver was detected by real-time quantitative polymerase chain reaction using specific target primers for CYP450 genes. The level of protein expression of CYP2B1 was detected by Western blot.Results Compared with the control group,fructose significantly decreased the activity of CYP1A2,CYP2B6,CYP2C9,CYP2D6; ferulic acid significantly decreased the activity of CYP2C9,CYP2B6; ligustrazine significantly decreased the activity of CYP1A2,CYP2C9,CYP2B6; peoniflorin significantly decreased the activity of CYP2D6,CYP2B6; fructose,ferulic acid,peoniflorin inhibited the mRNA expression of CYP2B1; fructose,ferulic acid,ligustrazine and peoniflorin also inhibit the protein expression of CYP2B1.Conclusion Fructose,ferulic acid,peoniflorin inhibit the activity of CYP2B1,decrease the expression levels of mRNA and protein of CYP2B1.