芬苯达唑前药的体外代谢研究  

In vitro Metabolism of Fenbendazole Prodrug

作　　者：温爱丹[1] 段李平[1] 刘丛珊[1] 陶奕[1] 薛剑[1] 吴宁波[1] 姜斌[1] 张皓冰[1] 

机构地区：[1]中国疾病预防控制中心寄生虫病预防控制所、世界卫生组织疟疾、血吸虫病和丝虫病合作中心、卫生部寄生虫病原与媒介生物学重点实验室,上海200025

出　　处：《中国寄生虫学与寄生虫病杂志》2013年第1期68-70,共3页Chinese Journal of Parasitology and Parasitic Diseases

摘　　要：以人工胃液、人工肠液和小鼠肝匀浆为体外模型,采用高效液相色谱法,对合成的芬苯达唑前药MPT在上述3种生物基质中的代谢进行定量研究,绘制代谢曲线,并测定其对细粒棘球蚴原头节的杀伤作用。结果表明,芬苯达唑前药在人工胃液、人工肠液和小鼠肝匀浆中均可发生代谢,在肝脏匀浆中代谢为有活性的芬苯达唑,代谢率为7.92%。在10μg/ml芬苯达唑前药的体外作用下,细粒棘球蚴原头节死亡率为45.9%。Synthesized fenbendazole prodrug N-methoxycarbonyl-N＇-（2-nitro-4-phenylthiophenyl） thiourea （MPT） was analyzed in vitro in artificial gastric juice, intestinal juice and mouse liver homogenate model by using HPLC method, and metabolic curve was then generated. MFT was tested against Echinococcus granulosus protoscolices in vitro. The result showed that MPT could be metabolized in the three biological media, and to the active compound fenbendazole in liver homogenate, with a metabolic rate of 7.92%. Besides, the prodrug showed a weak activity against E. granulosus protoscolices with a mortality of 45.9%.

关 键 词：芬苯达唑前药 体外代谢 棘球蚴 原头节 

分 类 号：R383.33[医药卫生—医学寄生虫学]