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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 .
Objective To prepare epirubicin (Epi) and its metabolites which can be hydrolyzed by β-glucuronidase (βG) .Methods Epi metabolites (urine of patients treated with Epi) After concentration and concentration under reduced pressure, the metabolites were separated and purified by RP-HPLC, and the metabolites were analyzed by MTT assay.Results The results of RP-HPL C (Peak-to-peak), and the external standard method confirmed that the sixth component (peak) was Epi. Cytotoxicity experiments confirmed that the first peak (component) to the fourth peak ΒG activation and killing effect.Conclusion Epi metabolites from 1 to 4 can be used as βG prodrugs.