刘建明 熊玉卿. 普伐他汀对灯盏乙素小鼠肝脏转运的作用及机制初探J. 药学学报, 2011,46(3): 269-273.
引用本文: 刘建明 熊玉卿. 普伐他汀对灯盏乙素小鼠肝脏转运的作用及机制初探J. 药学学报, 2011,46(3): 269-273.
LIU Jian-Meng, Xiong-Yu-Qing. Effect of pravastatin on transportation of scutellarin in mouse liver and its mechanismJ. 药学学报, 2011,46(3): 269-273.
Citation: LIU Jian-Meng, Xiong-Yu-Qing. Effect of pravastatin on transportation of scutellarin in mouse liver and its mechanismJ. 药学学报, 2011,46(3): 269-273.

普伐他汀对灯盏乙素小鼠肝脏转运的作用及机制初探

Effect of pravastatin on transportation of scutellarin in mouse liver and its mechanism

  • 摘要:

    从整体动物及细胞水平考察灯盏乙素在小鼠肝脏中的摄取转运, 研究其可能的跨膜转运机制。应用高效液相色谱法测定比较不同剂量普伐他汀预处理组小鼠空白小鼠间灯盏乙素的血药浓度、肝脏药物浓度等药动学性质的改变; 使用高效液相色谱法测定比较空白组肝细胞、oatp2高表达组肝细胞以及普伐他汀处理的oatp2高表达组肝细胞对灯盏乙素的摄取情况。结果发现, 普伐他汀灌胃能影响灯盏乙素的药动学特征, 灯盏乙素的血浆清除率CL降低, AUC增加; PCN诱导组肝细胞对灯盏乙素的摄取较空白组增加, 在同时加入普伐他汀时, 小鼠肝细胞对灯盏乙素的摄取减少。目前的研究认为普伐他汀和灯盏乙素之间可能存在潜在的药物相互作用, 可能是通过相互竞争oatp2介导的转运通路而发生, 这种通路存在于肝脏对灯盏乙素的摄取中。

     

    Abstract:

    This study is to investigate the transportation of scutellarin in cell and live models and study on mechanism of absorption and transport of scutellarin in mouse liver.  The concentration of scutellarin in plasma and liver from control and pretreated groups was determined by high performance liquid chromatography.  The uptake of scutellarin was examined in control hepatocytes group, induced hepatocytes group and induced hepatocytes plus pravastatin group.  Pravastatin can affect the pharmacokinetics of scutellarin in mouse: CL is decreased while AUC is increased.  The scutellarin absorption of hepatocyte induced group was higher than that of control group, but was decreased in the group with pravastatin added.  The research showed that there was potential drug interaction between pravastatin and scutellarin.  The drugs may compete for oatp2 mediated transport pathway consisted in the uptake of scutellarin in liver.

     

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