›› 2013, Vol. 31 ›› Issue (1): 17-68-70.

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In vitro Metabolism of Fenbendazole Prodrug

WEN Ai-dan,DUAN Li-ping,LIU Cong-shan,TAO Yi,XUE Jian,WU Ning-bo, JIANG Bin,ZHANG Hao-bing*   

  1. National Institute of Parasitic Diseases, Chinese Center for Disease Control and Prevention; Key Laboratory of Parasite and Vector Biology, MOH; WHO Collaborating Centre for Malaria, Schistosomiasis and Filariasis, Shanghai 200025, China
  • Online:2013-02-28 Published:2013-04-23

Abstract: 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. MPT 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%.

Key words: Fenbendazole prodrug, In vitro metabolism, Echinococcus granulosus, Protoscolex