注射用灯盏花素对大鼠CYP2D6体内代谢活性的影响

Effect of Breviscapinun Powder for Injection on the Activity of CYP2D6 in Rats

目的:研究灯盏花素对大鼠细胞色素P4502D6(CYP2D6)体内代谢活性的影响。方法:试验分为3组,即对照(生理盐水)和灯盏花素高、低剂量(0.54、0.18mg·100g-1)组,静脉注射给药,每天1次,连续14d。各组分别于第15天注射美托洛尔溶液,于给药前和给药后不同时间点眼内眦静脉取血0.8mL,使用高效液相色谱法测定血浆中美托洛尔的浓度。结果:静脉给予大鼠注射用灯盏花素14d后,灯盏花素高剂量组美托洛尔的AUC和t1/2显著高于对照组,CL显著低于对照组(P<0.05)。灯盏花素低剂量组虽然也有相同趋势,但无显著性差异。结论:高剂量注射用灯盏花素可显著抑制大鼠CYP2D6的体内活性。

OBJECTIVE： To study the effect of breviscapinun powder for injection on the activity of cytochrome P4502D6 （CYP2D6） in rats. METHODS： The rats were randomly divided into three groups, i.e. control group （normal saline）, breviscapinun low-dose and high-dose groups （0.54,0.18 mg·100 g^-1）. Each group was given medicine once a day via intravenous injection for 14 days. On the 15th day, all rats were injected with metoprolol solution, then blood samples of inner canthus 0.8 mL were collected at a set of time-points. The plasma concentration of metoprolol was determined by HPLC. RESULTS： In high-dose group, AUC and t1/2 of metoprolol were significantly higher than those in control group （P〈0.05）, and CL were significantly lower than that of control group （P〈0.05） 14 days after administration of breviscapinun powder for injection. Compared with control group, AUC and t1/2 of metoprolol were higher and CL was lower in low-dose group, but there were no significant differences between low-dose group and control group. CONCLUSION： High-dose of breviscapinun powder for injection can significantly inhibit the activity of CYP2D6 in rats.