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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 the scutellarin present in the plasma, bile, urine and feces of rats after intragastric administration of breviscapine. Methods Plasma, bile, urine and stool samples of rats in the administration group and blank group were comparatively analyzed by using gradient elution method by using HPLC in combination with photodiode array detector (DAD), and in the same liquid phase Chromatographic conditions and reference substance retention time and UV absorption characteristics were compared to identify the main metabolites. Results The metabolite scutellarein-6-O-β-D-glucuronide (M5) was identified from plasma of rat ig20,200mg / kg breviscapine ; The metabolite scutellarein-6,7-O-β-D-glucuronide (scutellarein-6,7-di-O-β) was identified from the bile of rat breviscapine 200mg / -D-glucuronide, M1), 6-O-methyl-scutellarin (M3), scutellarein-6 O-β-D-glucuronide (M5) and scutellarin (M7) were isolated from the urine of rat breviscapine 20mg / kg. The metabolites baicalein-6,7- O-β-D-glucoside (scutellarein-6,7-di-O-β-D-glucuronide, M1) from the rat ig200mg / Scutellarein-6,7-di-O-β-D-glucuronide (M1), scutellarein (M2) and scutellarin scutellarin, M7). The metabolite scutellarein (M2) was identified from the feces of 200 mg / kg breviscapine in rats. Conclusion Scutellarin is widely metabolized in rats and mainly exists in the form of its metabolites. The metabolites produced by Scutellarin in rats are mainly excreted through urine and bile.