| 摘要: |
| ［摘要］目的 探讨去氢钩藤碱与异去氢钩藤碱在大鼠体内的生物转化．方法 去氢钩藤碱、异去氢钩藤碱对大鼠经口投药30 min内收集到的胆汁样品进行高效液相色谱串联质谱仪（LC-MS）测定．结果 发现去氢钩藤碱的底物和2个I相代谢物、2个II相代谢物可以检出，而异去氢钩藤碱的I相代谢物没有检出，但II相代谢物检出4个．结论 分析结果显示这2个四环氧化吲哚生物碱的代谢与钩藤碱、异钩藤碱的肝脏代谢非常相似，并且都存在经口投药之后的肝首过效应．体外实验验证了以上代谢过程的结论，并显示是肝微粒体酶CYP450对去氢钩藤碱、异去氢钩藤碱在肝脏的生物转化起催化作用． |
| 关键词: ［关键词］去氢钩藤碱 异去氢钩藤碱 生物转化 代谢 |
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| Biotransformation of Corynoxeine and Isocorynoxeine in Rats |
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HUANG Min－Jie
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| Abstract: |
| ［Abstract］Objective To investigate the biotransformation of Corynoxeine and Isocorynoxeine in Rats． Methods Corynoxeine and isocorynoxeine were administered orally to rats， and the bile samples of rats were collected to analyze by LC-MS．Results It was found for the bile samples taken for first 30 mins that two phase I metabolites and two phase II ones were detected for corynoxeine by LC-MS．However for isocorynoxeine there were 4 phase II metabolites found but no phase I ones in the same sample．Conclusions There is a hepatic first-pass effect after their oral administration. According to analysis of samples in vivo and in vitro by LC-MS and comparison with the fate of rhynchophylline and isorhynchophylline in rats，corynoxeine and isocorynoxeine seem to have a similar biotransformation．Also incubation of the substrates with rat liver microsomes show that CYP450 plays a key role in their metabolic catalysis. |
| Key words: ［Key words］Corynoxeine Isocorynoxeine Biotransformation Metabolism |