灯盏花素对大鼠CYP3A4体内活性的影响  

Effect of Breviscapinum on the Activity of CYP3A4 in Rats

作　　者：刘洁[1] 韩晓文[1] 李芹[1] 焦建杰[1] 高思楠[1] 孟素蕊[1] 娄建石[1] 

机构地区：[1]天津医科大学基础医学院,天津300070

出　　处：《时珍国医国药》2011年第9期2082-2084,共3页Lishizhen Medicine and Materia Medica Research

基　　金：天津市自然科学基金重点项目(No.09JCZDJC21500);高等学校博士学科点专项科研基金(新教师基金)资助课题(No.20091202120012)

摘　　要：目的以咪达唑仑作为探针药物,研究灯盏花素对大鼠细胞色素P450 3A4(CYP3A4)体内活性的影响,为临床合理用药提供参考。方法将SD大鼠随机分为3组,对照组、灯盏花素低剂量组和高剂量组。低剂量组和高剂量组每天分别尾静脉给予灯盏花素粉针剂0.18 mg/100 g及0.54 mg/100 g,共10 d,对照组给予生理盐水。各组分别于第11天注射咪达唑仑溶液,于给药前及给药后不同时间点眼内眦静脉取血0.8 ml,使用高效液相色谱(HPLC)法测定血浆中咪达唑仑的浓度。结果静脉给予大鼠灯盏花素粉针剂10 d后,与对照组相比,低剂量组和高剂量组咪达唑仑的AUC、MRT和tφ均显著高于对照组(P<0.05),CL显著低于对照组(P<0.05);灯盏花素高剂量组与低剂量组无显著性差异。结论灯盏花素可明显抑制大鼠CYP3A4的体内活性。Objective To study the effect of breviscapinum on the activity of CYP3A4 in rats with midazolam as probe. Methods The rats were randomly divided into three groups： control group,low-dose group and high-dose group.The rats in the low-dose group and high-dose group were treated with breviscapinum powder injection by caudal vein at the dose of 0.18 mg/100g and 0.54mg/100g once a day for 10 days respectively,the rats in the control group were injected with normal saline.On the 11th day,all rats in each group were injected midazolam,then venous blood samples were collected at a set of timepoints.The plasma concentration of midazolam was determined by HPLC. Results In low-dose group and high-dose group,AUC,MRT and t1/2 of Midazolam were significantly higher than those of control group（P0.05）,and CLs was significantly lower than that of control group（P0.05）.There was no significant difference between low-dose group and high-dose group（P0.05）. Conclusion Breviscapinum can significantly inhibit the activity of CYP3A4 in rats.

关 键 词：灯盏花素 咪达唑仑 大鼠 

分 类 号：R285.5[医药卫生—中药学]