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研究抗人肝细胞癌单克隆抗体Fab片段修饰物的99mTc标记方法。用2亚氨基噻吩盐酸盐(IT)修饰HAb18Fab片段。用99mTcGH转络合法标记ITFab,测定标记物的放化纯度及生物活性,进行荷人肝癌裸鼠模型的放射免疫显像。结果:纸层析法测得标记率为50%~80%,体外细胞结合法测定免疫活性为30%~40%。荷人肝癌裸鼠模型尾静脉注入99mTcITFab后4~8小时,肿瘤区放射性有浓聚,12~22小时浓聚最多,T/NT值为518~748。因此,99mTcITFab可特异性浓聚于荷人肝癌裸鼠模型中,可能成为肝癌放射免疫显像的有效显像剂。
A 99mTc labeling method for anti-human hepatocellular carcinoma monoclonal antibody Fab fragment modification was studied. The HAb 18 Fab fragment was modified with 2-iminothiophene hydrochloride (IT). The IT-Fab was labeled with 99mTc-GH complexation method. The radiochemical purity and biological activity of the marker were measured. Radioimmunoimaging of the human hepatocellular carcinoma nude mouse model was performed. Results: The labeling rate of paper chromatography was 50% to 80%, and the in vitro cell binding assay was 30% to 40%. Intratumor injection of 99mTc-IT-Fab into the tail vein of a human hepatocellular carcinoma nude mouse model was performed for 4 to 8 hours. The radioactivity in the tumor area was concentrated, and the concentration was highest in 12 to 22 hours. The T/NT value was 5 to 18 to 7 to 48. Therefore, 99mTc-IT-Fab can be specifically concentrated in a human hepatoma bearing nude mouse model, and may be an effective imaging agent for liver cancer radioimmunoimaging.