【摘要】 目的　制备可被β-葡萄糖醛酸苷酶 (βG)水解活化的表阿霉素 (Epirubicin,Epi)及其代谢物 .方法　 Epi代谢物(Epi治疗患者的尿液 )经 C1 8树脂初提富集并减压蒸溜浓缩后 ,用反相高效液相色谱法 (RP- HPL C)分离纯化代谢物组分 ,用 MTT法分析 βG对代谢物组分的激活杀伤作用 .结果　经 RP- HPL C洗脱分离 ,共得到 6个组分 (峰 ～峰 ) ,外标法证实第 6组分 (峰 )为 Epi.细胞毒实验证实第 1组分(峰 )至第 4组分 (峰 )均有βG激活杀伤作用 .结论　 Epi代谢物第 1至第 4组分均可作为 βG的前体药物 .更多还原

【Abstract】 AIM To find a simple and rapid method for the preparation of β glucuronidase prodrug epirubicin metabolite from epirubicin treated patient urine. METHODS The urine of the patients treated with epirubicin within 48 hours was enriched and concentrated by C18 resin and then purified by reversed phase high performance liquid chromatography (RP HPLC) with the column packed with YWG C18. The mobile phase consisted of acetonitrile 0.15 mmol·L -1 NaH 2PO 4/2 mmol·L -1 triethyamine (pH 3.5) (1∶4 V/V ), and it was detected by UV detector at a wavelength of 590 nm. MTT assay was used to analyze cytotoxicity for each component peak. RESULTS Six eluted peaks were obtained and the sixth peak was proved as Epi. by outside standard method. MTT assay showed that the peak Ⅰ to peak Ⅳ had β Glucuronidase active killing effects, and it had positive relation with the component concentration. CONCLUSION Peak Ⅰ to peak Ⅳ can be used as prodrug of β glucuronidase for ADEPT.更多还原