莪术油对大鼠肝微粒体CYP1A2酶活性的影响

Evaluations of Zedoary Turmeric Oil on the Activity of Rat CYP1A2

目的:建立非那西丁及其代谢产物的液质联用检测法,研究莪术油对大鼠肝微粒体CYP1A2酶活性的影响,为临床合理用药提供参考。方法:色谱柱为XDB-C18(150mm×2.1mm,5μm),流动相为乙腈-0.1%甲酸,流速:0.4mL.min-1,柱温:30℃,以多反应监测方式采集数据。以非那西丁为探针药物,采用体外实验,实验组给予莪术油,对照组给予生理盐水,评价药物代谢酶CYP1A2酶活性的变化。结果:非那西丁和对乙酰氨基酚的检测浓度线性范围分别为4～1600ng.mL-1(r=0.9973)、3-2000ng.mL-1(r=0.9973)。实验组测得的扑热息痛/非那西丁的比值:11.30±0.71,对照组:9.60±1.04,t检验显示P<0.05,有统计学意义。结论:本法可用于检测大鼠肝微粒体孵育液中非那西丁及其代谢物浓度。莪术油对大鼠肝CYP1A2酶的活性,有体外诱导作用。

Objective： To develop an HPLC - MS determination method of phenacetin and paracetarnol and to investi- gate the effect of Zedoary Turmeric oil on the activity of rat CYP1A2 for providing reference to rational drug use in clinic. Methods ： Samples were separated on XDB - CIs （ 150ram x 2.1 ram, 5 p.m） column, acetonitrile - 0. 1% formic acid was used as mobile phrase, and the flow rate was 0.4 mL ·min-1 ,the column temperature was 30cC. The multiple reaction monitor was adopted to detect the concentration of phenacetin and paracetamol. Phenacetin was used as a probe of CYPlA2. The activity of rat CYPIA2 was evaluated by an in - vitro experiment which two group involved, experiment group was given Zedoary Turmeric oil and the control group was ~iven saline. Results： The calibration curves were linear in the ranges of 4 ~1600ng ~ mL-^（ r =0.9973） phenaeefin and 3～2000ng · mL-1 （ r =0.9973） paracetaraol. The ratio of paraeetamol/phenacetin in experiment group was 11.30 ＋ 0.71, the ratio of control group was 9.60±1.04, pair T test was P 〈 0.05. Conclusion： The method is suitable for determination of phenacetin and paracetamol in rat liver mierosomal ineubatlon system. The activity of rat liver CYP1 A2 can be enhanced by Zedoary Turmerle oil.