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[目的]探讨99mTc标记的端粒酶靶向小干扰RNA(siRNA)在肝肿瘤细胞中的摄取情况,以期将来用于体内肿瘤显像。[方法]通过双功能螯合剂用99mTc标记hTERT靶向和对照siRNA探针,测定6h内血清放化纯,比较脂质体转染和非转染条件下两组的HepG2细胞摄取率。[结果]99mTc标记的siRNA在室温和37℃条件下具有很好的血清稳定性(放化纯>94%)。实验与对照组探针的HepG2细胞摄取率均随着时间延长不断增加,且在脂质体转染条件下的细胞摄取较非转染高。[结论]hTERT靶向siRNA标记探针的血清稳定性高且可被肿瘤细胞特异摄取,具有潜在的体内肿瘤显像的应用价值。
[Objective] To investigate the uptake of 99mTc-labeled telomerase targeting small interfering RNA (siRNA) in liver tumor cells in the future for in vivo tumor imaging. [Method] The hTERT-targeting and control siRNA probes were labeled with 99mTc by bifunctional chelator and the serum levels were determined within 6h. The uptake rate of HepG2 cells was compared between the transfected and non-transfected lipofectin groups. [Results] 99mTc-labeled siRNA had good serum stability (radiochemical purity> 94%) at room temperature and 37 ℃. The uptake rate of HepG2 cells in both experimental and control groups increased with time, and the cell uptake under lipofection was higher than that of non-transfected cells. [Conclusion] hTERT target siRNA labeled probe has high serum stability and can be specifically taken up by tumor cells, and has the potential value of in vivo tumor imaging.