阳春砂仁和化橘红对小鼠肝脏CYP3A及肠道首过效应的影响  

Influence of Amomum Villosum Lour and Exocarpium Citrl Grandis on Liver CYP3A and Intestinal First Pass Effect in Mice

作　　者：王永辉 奇锦峰[2] 林梅[2] 孔永红 

机构地区：[1]驻马店市中心医院药剂科,河南驻马店463000 [2]广州中医药大学中药学院,广东广州510006

出　　处：《中国执业药师》2015年第12期34-38,共5页China Licensed Pharmacist

摘　　要：目的:研究阳春砂仁和化橘红对小鼠肝脏CYP3A以及肠道首过效应的影响,以指导临床精细用药。方法:将小鼠分为纯水对照组(10 m L/kg),酮康唑(1.8 mg/kg)、阳春砂仁和化橘红高、低剂量组(30 m L/kg和10 m L/kg)。灌胃给药2次/d,连续3 d。以分光光度法测定血中对乙酰氨基酚浓度;用超速离心法分离小鼠肝微粒体;分光光度法检测微粒体中CYP3A活性。结果:以红霉素和氨基比林为底物测定肝脏CYP3A活性时,阳春砂仁和化橘红高、低剂量组与纯水对照组之间均无显著性差异(P>0.05);血中APAP浓度测定结果显示,阳春砂仁和化橘红高、低剂量组显著高于纯水对照组(P<0.01或P<0.05);P-gp偶联的ATP酶活性测定结果显示,阳春砂仁和化橘红高、低剂量组明显低于纯水对照组(P<0.01或P<0.05)。结论:阳春砂仁和化橘红对小鼠肝脏CYP3A的活性均没有抑制或诱导作用,对小鼠肠道P-gp活性具有不同程度的抑制作用。Objective ： To investigate the influence of amomum villosum lour and exocarpium citrl grandis on liver CYP3 A and intestinal first pass effect in mice so as to guide the clinical drug use. Methods ： The mice were randomly divided into control（pure water,10 m L/kg）,ketoconazole（1.8 mg/kg） as well as high（30 m L/kg）and low（10 m L/kg） dose amomum villosum lour and exocarpium citrl grandis groups,and treated with the corresponding drugs by lavage,2 times a day for 3 d. The concentration of acetaminophen in serum was determined by spectrophotometry. The microsome was separated from mouse liver by ultracentrifugation,in which the activity of CYP3 A was determined by spectrophotometry. Results ： The CYP3 A activity in liver determined using erythromycin and aminopyrine as the substrates showed no significant difference in high and low dose amomum villosum lour and exocarpium citrl grandis groups and in control group（P〈0.05）. However,the APAP concentrations in high and low dose amomum villosum lour and exocarpium citrl grandis groups were significantly higher,while the activity of P-gp coupled ATPase was significantly lower,than those in control group（P〈0.05 or P〈0.01）. Conclusion ： Amomum villosum Lour and exocarpium citrl grandis showed no inhibitory or inducing effect on the activity of CYP3 A in mouse liver,while showed a certain inhibitory effect on intestinal P-gp activity in mice.

关 键 词：CYP3A P-糖蛋白 阳春砂仁 化橘红 

分 类 号：R394[医药卫生—医学遗传学]