摘要
目的以咖啡因作为探针药物,研究苦参对大鼠细胞色素P450 1A2(CYP1A2)体内代谢活性的影响。方法将Wistar大鼠随机分为4组:空白对照组、苦参组(实验组)、苯巴比妥组(诱导剂阳性对照组)和西咪替丁组(抑制剂阳性对照组)。苦参组,灌胃给予苦参溶液100 mg.kg-1;空白对照组,灌胃给予与苦参组体积相同的生理盐水;苯巴比妥组,腹腔注射苯巴比妥注射液50 mg.kg-1;西咪替丁组,每日腹腔注射西咪替丁注射液50 mg.kg-1,各组均为每日1次,连续5 d。第6 d,各组大鼠均经尾静脉注射咖啡因溶液2.5 mg.kg-1,于给药前及给药后不同时间,眼内眦静脉取血0.8 mL,用高效液相色谱法,测定血浆中咖啡因的浓度。结果给予大鼠苦参5 d后,苦参组的咖啡因AUC、MRT、Cmax明显低于空白对照组和西咪替丁组(P<0.05),明显高于苯巴比妥组(P<0.05);而CL明显高于空白对照组和西咪替丁组(P<0.05)而明显低于苯巴比妥组(P<0.05)。结论苦参可明显诱导大鼠CYP1A2的体内代谢活性;但诱导强度低于苯巴比妥。
Objective To study the effect of Sophora flavescens on the metabolic activity of cytochrome P4501A2（CYP1A2） in rats with caffeine as probe.Methods The rats were randomly divided into four groups： blank control group,Sophora flavescens group（test group）,phenobarbital group（induction control group） and cimetidine group（inhibition control group）.Sophora flavescens were administered orally for five days at a dose of 100 mg·kg-1 body weight for Sophora flavescens group and normal saline were administered orally for blank control group at the same volume as Sophora flavescens group.Sodium phenobarbital and cimetidine injection were administered intraperitoneally for five days at a dose of 50 mg·kg-1 body weight for phenobarbital group and cimetidine group,respectively.On the 6th day,all rats in each group were injected caffeine 2.5 mg·kg-1,then venous blood samples were collected at a set of time-points.The plasma concentrations of the caffeine were determined by HPLC.Results In Sophora flavescens group,AUC,MRT and Cmax of caffeine were significantly lower than those of blank control group and cimetidine group（P〈0.05） and were significantly higher than those of phenobarbital group（P〈0.05）,and CL was significantly higher than that of blank control group and cimetidine group（P〈0.05） and was significantly lower than that of phenobarbital group（P〈0.05）.Conclusion Sophora flavescens can significantly induce the metabolic activity of CYP1A2 in rats,but the effect of induction is weaker than phenobarbital.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2011年第10期773-776,共4页
The Chinese Journal of Clinical Pharmacology
基金
天津市自然科学基金重点资助项目(09JCZDJC21500)
高等学校博士学科点专项科研基金(新教师基金)资助项目(20091202120012)
