【摘要】 目的:探讨铼-188(188Re)标记前列腺特异膜抗原单克隆抗体7E11C5.3(188Re-7E11C5.3)对前列腺癌细胞系LNCaP的体外抑制作用。方法:采用2-巯基乙醇直接还原法制备188Re-7E11C5.3标记物,纸层析法测定标记率和放化纯度,直线回归外推法测定免疫活性分数。四唑盐(MTT)法测定其体外细胞毒作用。结果:188Re-7E11C5.3的标记率为(93.16±2.18)%,放化纯度为(95.62±0.48)%,免疫活性分数为(74.86±1.86)%。188Re-7E11C5.3对LNCaP细胞的生长抑制作用明显强于188Re标记的正常鼠IgG(mIgG)和游离188ReO4-,其半数有效抑制浓度(IC50)分别为(23.38±3.73)×107Bq/L,(59.21±8.02)×107Bq/L和(68.89±10.91)×107Bq/L。结论:188Re-7E11C5.3能有效抑制体外培养LNCaP细胞的增殖,可用于前列腺癌的放射免疫治疗。更多还原

【Abstract】 AIM: To investigate the effect of 188Re labeled monoclonal antibody on prostatic specific membrane antigen 7E11C5.3,radioimmunotherapy for the treatment of human prostate cancer cell line LNCaP in vitro.METHODS: 188Re-7E11C5.3 was prepared by direct 2-mercaptoethanol reduction method.Labeling efficiency and radiochemical purity was measured by paper chromatography.Immunoreactive fraction was determined by linear extrapolation.Cytotoxicity to LNCaP cells was determined by MTT assay.RESULTS: The labeling yield of 188Re-7E11C5.3 was(93.16±2.18)%,the radiochemical purity was(95.62±0.48)%,and the immunoreactive fraction was(74.86±1.86)%.The inhibitory effect of 188Re-7E11C5.3 on cell proliferation of LNCaP cells was significantly higher than that of 188Re-mIgG or 188ReO-4.The 50% inhibitory doses(IC50) of 188Re-7E11C5.3,188Re-mIgG,and 188ReO-4 were(23.38±3.73)×107 Bq/L,(59.21±8.02)×107 Bq/L and(68.89±10.91)×107 Bq/L,respectively.CONCLUSION: 188Re-7E11C5.3 can effectively inhibit the growth of in vitro cultured prostate cancer cells and shows much potential for prostate cancer radioimmunotherapy.更多还原