探索用^99Tc^m直接标记表皮生长因子(EGF)的方法并研究其在荷C6动物体内的生物学分布特点。巯基乙醇(20 mL/L)10μL还原EGF(2.5μg);含0.5μg SnCl2的亚甲基二膦酸盐(MDP)溶液将还原高价锝使之与还原EGF的巯基结合,放化纯度大于95%,标记物稳定性较好,在6 h内放化纯度大于95%。通过内皮细胞培养进行^99Tc^m-EGF的生物活性鉴定,显示EGF在锝标记前后生物学活性未见明显改变(P〉0.05).^99Tc^m-EGF在荷瘤鼠体内生物学分布显示肝、脾、肾等组织放射性分布较高,瘤区放射性较高,而脑组织最低,4 h瘤与正常组织放射性摄取比值(Tumor/Normal Tissue)为2.25,SPECT全身显像显示瘤组织放射性核素浓聚。因此直接合成的^99Tc^m-EGF可望成为特异性诊断高表达EGFR肿瘤的SPECT分子显像剂。
The method of technetium-99m direct radiolabeling of epidermal growth factor (EGF) and the biological distribution characteristics of ^99 Tc^m-EGF in C6-bearing rats were ex- plored. Following reduction of EGF(2.5 μg) with 2-ME(20 mL/L, 10 μL), EGF was labeled with ^99Tc^m in the presence of SnC12 (0.5 μg). The results show that radiochemical purity of ^99Tc^m-EGF is more than 95% and ^99Tc^mEGF is of the characteristic of stability. The biological activity analyzed by the culture of endothelial cells shows that there is no significant difference between ^99Tc^m-EGF and EGF(P〉0.05). Biological distribution is observed at different time point after injection of ^99Tc^m-EGF into tumor-bearing Wistar rats, and shows ^99Tc^m-EGF is mainly accumulated in liver, kidney and spleen and least accumulated in the brain. Tumor take relatively high concentration of ^99Tc^m-EGF and the uptake ratio of tumor to normal tissue is 2.25 at 4 h. So ^99 Tc^m-EGF prepared by this direct method appears to be a feasible way to detect the tumors expressing high EGFR(such as glioma).