大鼠肝微粒体中钩吻素子UPLC-MS/MS法测定与酶促反应动力学研究
李彧曾荣洁郑雪卿郭陈建忠
福建中医药大学药学院
Abstract: 目的建立UPLC-MS/MS法测定大鼠肝微粒体中钩吻素子的浓度及其酶促反应动力学研究。方法优化钩吻素子与肝微粒体的反应体系,采用UPLC BEH C18色谱柱,流动相为甲醇-水（两者均含0.1%甲酸）,梯度洗脱,流速为0.3 mL/min,进样量为1μL,质谱采用正离子,MRM模式检测孵育体系中钩吻素子的浓度,并应用Linewearve-Burk作图分析数据,计算酶促动力学常数。结果钩吻素子在0.5～30μM范围内线性良好,回归方程为y=0.1544x-0.0593（r=0.9939,n=5）。钩吻素子的酶促反应动力学参数Km为14.2μmol/L,Vmax为303.03pmol/（min.mg.pro）以及肝清除率CLint（Vmax/Km）为21.37μL/（min.mg.pro）。结论该方法简单、快速、可靠,适应于钩吻素子的体外代谢研究。
- DOI：
10.13260/j.cnki.jfjtcm.010572
- Series：
- Subject：
- Classification Code：
R285.5
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