戊己丸不同配比方对大鼠体外CYP1A2酶活性的影响  

Effects of Wuji Pill with different compatibility on the activity of cytochrome P450 1A2 in rat liver microsomes in vitro

作　　者：翁小刚[1] 李玉洁[1] 杨庆[1] 梁日欣[1] 王怡薇[1] 刘晓霓[1] 韩晓[1] 张甘霖[2] 隋峰[1] 朱晓新[1] 

机构地区：[1]中国中医科学院中药研究所,北京市100700 [2]北京中医药大学,北京市100029

出　　处：《世界华人消化杂志》2010年第6期586-591,共6页World Chinese Journal of Digestology

基　　金：国家自然科学基金重点课题基金资助项目;No.30930114;No.90709017;国家科技支撑计划(十一五)项目子课题基金资助项目;No.2006BAI08B04-4;国家中医药管理局中医药行业科研专项基金资助项目;No.200807036;中国中医科学院自主选题基金资助项目;No.ZZ2006102~~

摘　　要：目的:探讨戊己丸不同配比方对大鼠体外肝微粒体CYP1A2酶活性的影响,从"中药配伍-代谢"关系探讨中药配伍机制.方法:按L9(34)正交表,戊己丸的配比设计为9个受试复方,以非那西丁为探针药,HPLC检测戊己丸对大鼠体外肝微粒体CYP1A2酶活性的影响.结果:黄连、吴茱萸、白芍提取物及戊己丸方1-9抑制CYP1A2的生药IC50分别为:28.07、989.69、6633.28、57.92、104.38、321.28、32.17、80.09、71.47、76.76、40.41、29.45mg/L;黄连及戊己丸可以显著抑制CYP1A2酶活性,不同配比戊己丸抑制CYP1A2酶活性作用不同,有统计学差异;随着黄连、吴茱萸两药在戊己丸方中剂量水平的增高,戊己丸组方抑制CYP1A2酶活性的能力增强,随着白芍在戊己丸方中剂量水平的增高可以减弱该组方抑制CYPA2酶活性的能力,且戊己丸组方中吴茱萸和白芍配比不同可以影响方中黄连抑制CYP1A2酶活性的程度.结论:戊己丸配比不同,对CYP1A2酶活性的抑制作用不同,这种差异可能是不同配比戊己丸药效学、药动学差异的原因所在.AIM： To investigate the effects of Wuji Pill with different compatibility on the enzymatic activity of cytochrome P450 1A2 （CYP1A2） in rat liver microsomes in vitro. METHODS： Using phenacetin as a substrateprobe, the effects of Wuji Pill with different compatibility （No.1-9） on the enzymatic activity of CYP1A2 were detected by high-performance liquid chromatography （HPLC）. RESULTS： The half maximal inhibitory concentrations （IC50） of Rhizoma Coptidis, Fructus Evodiae Rutaecarpae, Radix Paeoniae Alba and Wuji Pill （No.1-9） on the enzymatic activity of CYP1A2 were 28.07, 989.69, 6633.28, 57.92, 104.38, 321.28, 32.17, 80.09, 71.47, 76.76, 40.41 and 29.45 mg/L, respectively. Rhizoma Coptidis and Wuji Pill （No.1-9） could significantly suppress the enzymatic activity of CYP1A2. The suppressive effects of Rhizoma Coptidis in Wuji Pill on the activity of CYP1A2 depend on the proportion of Fructus Evodiae Rutaecarpae and Radix Paeoniae Alba in Wuji Pill. With the increase in the proportion of Rhizoma Coptidis and Fructus Evodiae Rutaecarpae in Wuji Pill, the suppressive effects of Wuji Pill on the activity of CYP1A2 were strengthened. With the increase in the proportion of Radix Paeoniae Alba in Wuji Pill, the suppressive effects of Wuji Pill on the activity of CYP1A2 was weakened. CONCLUSION： Wuji Pill with different compatibility shows different suppressive effects on the enzymatic activity of CYP1A2. This may explain why Wuji Pill with different compatibility has different pharmacodynamic and pharmacokinetic characteristics.

关 键 词：戊己丸 CYP1A2 非那西丁 高效液相色谱法 中药 

分 类 号：R285.5[医药卫生—中药学]