Chen S, Liu L, Yang Y, Dai Z, Zeng F
Institute of Clinical Pharmacology, Tongji Medical University, Wuhan 430030.
J Tongji Med Univ. 2000;20(3):253-6. doi: 10.1007/BF02887006.
To study the metabolism of dauricine in vivo and in vitro and identify the structure of its main metabolites, urine of rats after drug administration as the samples of dauricine metabolism in vivo was studied. Rat liver S9 fraction was prepared and the oxygenation metabolism system reconstituted to perform phase I reaction of dauricine in vitro. TLC, HPLC-DAD and MS were used to analyze and identify dauricine and its main phase I metabolites in the samples. The results showed that besides the untransformed dauricine, in the urine samples there was little product of X' which had the same features of TLC, HPLC-DAD and MS as those of N-desmethyl dauricine (N-ddau). Part of dauricine could be transformed to a main metabolite X after incubating with S9 fraction in appropriate conditions. The molecular ion peak of X was m/z 611. The full scan MS2 spectrum of m/z 611 peak from S9 sample were m/z 580, m/z 566, m/z 552, m/z 206, which were same as those of N-ddau. Liver is the major organ for dauricine metabolism and part of dauricine is biotransformed by liver. The major metabolite is considered to be N-ddau.
为研究蝙蝠葛碱在体内外的代谢情况并鉴定其主要代谢产物的结构，以给药后大鼠尿液作为蝙蝠葛碱体内代谢的样本进行研究。制备大鼠肝脏S9组分并重建加氧代谢系统，以进行蝙蝠葛碱的体外I相反应。采用薄层层析（TLC）、高效液相色谱-二极管阵列检测（HPLC-DAD）和质谱（MS）对样本中的蝙蝠葛碱及其主要I相代谢产物进行分析和鉴定。结果表明，除未转化的蝙蝠葛碱外，尿液样本中几乎没有与去甲基蝙蝠葛碱（N-ddau）具有相同TLC、HPLC-DAD和MS特征的X'产物。在适当条件下，蝙蝠葛碱与S9组分孵育后，部分可转化为主要代谢产物X。X的分子离子峰为m/z 611。来自S9样本的m/z 611峰的全扫描二级质谱为m/z 580、m/z 566、m/z 552、m/z 206，与N-ddau的相同。肝脏是蝙蝠葛碱代谢的主要器官，部分蝙蝠葛碱经肝脏生物转化。主要代谢产物被认为是N-ddau。
