目的对大鼠灌胃灯盏花素后收集的血浆、胆汁、尿液以及粪便中存在的灯盏乙素的代谢产物进行鉴定。方法通过使用HPLC结合光电二极管阵列检测器(DAD),采用梯度洗脱的方法,对比分析给药组大鼠和空白组大鼠的血浆、胆汁、尿液以及粪便样品,并且在相同的液相色谱条件下与对照品的保留时间和紫外吸收特征进行对照来鉴定主要代谢产物。结果从大鼠ig20、200mg/kg灯盏花素的血浆中鉴定了代谢产物野黄芩素-6-O-β-D-葡萄糖醛酸苷(scutellarein-6-O-β-D-glucuronide,M5);从大鼠ig20、200mg/kg灯盏花素的胆汁中鉴定了代谢产物野黄芩素-6,7-O-β-D-二葡萄糖醛酸苷(scutellarein-6,7-di-O-β-D-glucuronide,M1)、6-O-甲基-灯盏乙素(6-O-methyl-scutellarin,M3)、野黄芩素-6-O-β-D-葡萄糖醛酸苷(scutellarein-6-O-β-D-glucuronide,M5)和灯盏乙素(黄芩素苷,scutellarin,M7),从大鼠ig20mg/kg灯盏花素的尿液中鉴定了代谢产物野黄芩素-6,7-O-β-D-二葡萄糖醛酸苷(scutellarein-6,7-di-O-β-D-glucuronide,M1),从大鼠ig200mg/kg灯盏花素的尿液中鉴定了代谢产物野黄芩素-6,7-O-β-D-二葡萄糖醛酸苷(scutellarein-6,7-di-O-β-D-glucuronide,M1)、野黄芩素(scutellarein,M2)和灯盏乙素(scutellarin,M7);从大鼠ig200mg/kg灯盏花素的粪便中鉴定了代谢产物野黄芩素(scutellarein,M2)。结论灯盏乙素在大鼠体内发生了广泛的代谢,并且主要以其代谢产物的形式存在;灯盏乙素在大鼠体内产生的代谢产物主要通过尿液和胆汁排泄。

Objective To identify the metabolites of scutellarin in plasma,bile,urine,and faeces samples of rats after ig administered with breviscapine.Methods To compare the plasma,bile,urine,and feces samples of rats after ig administered with breviscapine with those of rats of control groups by HPLC-DAD in a gradient elution way and identify the major metabolites by comparing their retention time and UV absorption with those of standard samples under the same HPLC conditions.Results Scutellarein-6-O-β-D-glucuronide (M5) was identified in rat plasma samples after ig administered with 20 mg/kg and 200 mg/kg breviscapine respectively;Scutellarein-6,7-di-O-β-D-glucuronide (M1),6-O-methyl-scutellarin (M3),scutellarein-6-O-β-D-glucuronide (M5),and scutellarin (M7) were identified in rat bile samples after ig administered with both 20 and 200 mg/kg breviscapine;Scutellarein-6,7-di-O-β-D-glucuronide (M1) was identified in rat urine sample after ig administered with 20 mg/kg breviscapine,and scutellarein-6,7-di-O-β-D-glucuronide (M1) associated with scutellarein (M2) and scutellarin (M7) were identified in rat urine sample after ig administered with 200 mg/kg breviscapine;Meanwhile,scutellarein (M2) was identified in rat feces sample after ig administered with 200 mg/kg breviscapine.Conclusion Scutellarin is metabolized extensively in rats after ig administered with breviscapine and the metabolites of scutellarin as the predominant form in vivo are mainly excreted in urine and bile of rats.

教育部博士点基金(200801630004)