Catto B A, Tracy J W, Webster L T
Mol Biochem Parasitol. 1984 Jan;10(1):111-20. doi: 10.1016/0166-6851(84)90023-9.
Niridazole, a nitro heterocyclic antischistosomal drug, is extensively metabolized to unknown metabolites by Schistosoma mansoni. We report that 1-thiocarbamoyl-2-imidazolidinone was isolated by high pressure liquid chromatography and identified by high resolution electron impact mass spectroscopy as a niridazole metabolite in schistosomes. After a 20-h in vitro incubation in 30 ml of medium containing 10 micrograms ml-1 [14C]niridazole (5.2 Ci mol-1), 100 S. mansoni worm pairs contained approximately 275 ng of 1-thiocarbamoyl-2-imidazolidinone. This amount represented 4% of the total metabolized fraction of niridazole in the parasite. Incubation of schistosomes with 1-thiocarbamoyl-2-[2 14C]imidazolidinone (2.7 Ci mol-1) indicated that this metabolite was not taken up. However, schistosomes released an average of 44 ng ml-1 or 1% of the total 1-thiocarbamoyl-2-imidazolidinone found in the worm back into 1 ml of medium during incubation. No host oxidative metabolites of niridazole were found in the parasites.
硝唑咪是一种硝基杂环抗血吸虫药物，被曼氏血吸虫广泛代谢为未知代谢产物。我们报告称，通过高压液相色谱法分离出了1-硫代氨基甲酰基-2-咪唑烷酮，并通过高分辨率电子轰击质谱法鉴定其为血吸虫体内的硝唑咪代谢产物。在含有10微克/毫升[14C]硝唑咪（5.2居里/摩尔）的30毫升培养基中进行20小时体外孵育后，100对曼氏血吸虫虫体含有约275纳克的1-硫代氨基甲酰基-2-咪唑烷酮。该量占寄生虫体内硝唑咪总代谢分数的4%。用1-硫代氨基甲酰基-2-[2 14C]咪唑烷酮（2.7居里/摩尔）孵育血吸虫表明该代谢产物未被摄取。然而，在孵育过程中，血吸虫平均将虫体内发现的1-硫代氨基甲酰基-2-咪唑烷酮总量的44纳克/毫升或1%释放回1毫升培养基中。在寄生虫体内未发现硝唑咪的宿主氧化代谢产物。
