白首乌中抗肿瘤活性成分告达庭-3-O-β-D-磁麻糖苷在大鼠体内的代谢产物分析

Studies on the Metabolites of Caudatin-3-O-β-D-Cymaropyranoside in Rats

    摘要
  • 摘要:
      目的   研究白首乌中甾苷成分告达庭-3-O-β-D-磁麻糖苷在大鼠体内的代谢情况。
      方法   大鼠单剂量灌胃给予20 mg/kg的告达庭-3-O-β-D-磁麻糖苷，分别收集24 h内的血浆、尿液、粪便和胆汁，样品经处理后，采用UPLC-Q-TOF分析，结合MetabolynxTM软件初步鉴定告达庭-3-O-β-D-磁麻糖苷在大鼠血浆、尿液、粪便和胆汁中的代谢产物。
      结果   在血浆、尿液、粪便和胆汁样品中发现了告达庭-3-O-β-D-磁麻糖苷的原型、水解及去甲基化代谢物，其中尿液中有原型，血浆和胆汁中有水解产物，粪便中有去2个甲基化产物，胆汁中有去1个和去3个甲基化产物。
      结论   告达庭-3-O-β-D-磁麻糖苷在大鼠体内可发生较为广泛的代谢，其中主要代谢类型有水解和去甲基化。

     

    Abstract:
      OBJECTIVE   To study the rats' metabolism of caudatin-3-O-β-D-cymarose glycosides, a kind of sterioside in Radix Cynanchi Auriculati.
      METHODS   Rats were given the a single dose of caudatin-3-O-β-D-cymarose glycosides by intragastric administration (20 mg/kg). Then the rats' plasma, urine, feces, and bile during the following 24 hours were collected. In addition, the processed samples were analyzed by UPLC-Q-TOF with MetabolynxTM software for the preliminary measurement of the metabolites of caudatin-3-O-β-D-cymarose glycosides in rats' plasma, urine, feces, and bile.
      RESULTS   The original, hydrolytic and demethylated metabolites of caudatin-3-O-β-D-cymarose glycosides were found in plasma, urine, feces, and bile samples, specifically, the original caudatin-3-O-β-D-cymarose glycosides in urine, hydrolytic metabolites in plasma and bile, two methylated metabolites in feces, along with one methylated and three demethylated metabolites in bile.
      CONCLUSION   The metabolism of caudatin-3-O-β-D-cymarose glycosides in rats is extensive, and the main types of metabolism are hydrolysis and demethylation.

     

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