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.
出处
《世界华人消化杂志》
CAS
北大核心
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~~
关键词
戊己丸
CYP1A2
非那西丁
高效液相色谱法
中药
Wuji Pill
CYP1A2
Phenacetin
High-performance liquid chromatography
Chinese medicine
