68Ga标记TMTP1探针在肝癌肿瘤模型中的microPET/CT显像研究

Study on microPET/CT imaging of 68Ga-labeled TMTP1 probe in HCC tumor model

目的研究68Ga[Ga]-NOTA-PEG2-TMTP1对SMMC-7721肝癌荷瘤小鼠模型的诊断效果.方法氨肽酶P2在一些肿瘤(如肝癌、肺癌、乳腺癌等)中有高表达.TMTP1可以特异性地靶向氨肽酶P2,本研究利用68Ga标记NOTA-PEG2-TMTP1合成68Ga[Ga]-NOTA-PEG2-TMTP1,然后对SMMC-7721肝癌荷瘤小鼠进行microPET/CT显像研究,研究其对肿瘤的诊断效果.结果68Ga[Ga]-NOTA-PEG2-TMTP1的放射性标记产率为(87.16±1.23)%,放化纯度大于99.0%.实验证明PEG修饰后的TMTP1,具有更好的肿瘤靶向性,肿瘤肌肉比可以高达5.66.结论对于肝癌的诊断来说,68Ga[Ga]-NOTA-PEG2-TMTP1可能是更好的PET探针,具有进一步临床转化的前景.

Objective To investigate the diagnostic effect of 68Ga[Ga]-NOTA-PEG2-TMTP1 on a mouse model of SMMC-7721 hepatocellular carcinoma in nude mice.Methods Aminopeptidase P2 was highly expressed in some tumors(e.g.,liver,lung,breast cancer,etc.).TMTP1 could specifically target aminopeptidase P2.In this study,68Ga[Ga]-NOTA-PEG2-TMTP1 was synthesized using 68Ga-labeled NOTA-PEG2-TMTP1,then SMMC-7721 hepatocellular carcinoma tumor-bearing nude mice for microPET/CT imaging study to investigate its diagnostic effect on tumors.Results The radiolabelling yield of 68Ga[Ga]-NOTA-PEG2-TMTP1 was(87.16±1.23)%,and the radiochemical purity was greater than 99.0%.It was demonstrated that TMTP1,after PEG modification,had better tumor targeting,with tumor muscle ratio up to 5.66.Conclusion For the diagnosis of hepatocellular carcinoma,68Ga[Ga]-NOTA-PEG2-TMTP1 may be a better PET probe with the prospect of further clinical translation.