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韩雪迪, 刘菲, 郭晓轶, 徐晓霞, 解清华, 刘特立, 朱华, 杨志. 正电子核素68Ga标记PSMA靶向分子探针在神经胶质瘤模型中的应用[J]. 肿瘤防治研究, 2018, 45(7): 447-452. DOI: 10.3971/j.issn.1000-8578.2018.17.0405
引用本文: 韩雪迪, 刘菲, 郭晓轶, 徐晓霞, 解清华, 刘特立, 朱华, 杨志. 正电子核素68Ga标记PSMA靶向分子探针在神经胶质瘤模型中的应用[J]. 肿瘤防治研究, 2018, 45(7): 447-452. DOI: 10.3971/j.issn.1000-8578.2018.17.0405
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HAN Xuedi, LIU Fei, GUO Xiaoyi, XU Xiaoxia, XIE Qinghua, LIU Teli, ZHU Hua, YANG Zhi. Application of 68Ga-PSMA-617 Molecular Probe for Micro-PET Imaging of Gliomas Model[J]. Cancer Research on Prevention and Treatment, 2018, 45(7): 447-452. DOI: 10.3971/j.issn.1000-8578.2018.17.0405
Citation: HAN Xuedi, LIU Fei, GUO Xiaoyi, XU Xiaoxia, XIE Qinghua, LIU Teli, ZHU Hua, YANG Zhi. Application of 68Ga-PSMA-617 Molecular Probe for Micro-PET Imaging of Gliomas Model[J]. Cancer Research on Prevention and Treatment, 2018, 45(7): 447-452. DOI: 10.3971/j.issn.1000-8578.2018.17.0405
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正电子核素68Ga标记PSMA靶向分子探针在神经胶质瘤模型中的应用

Application of 68Ga-PSMA-617 Molecular Probe for Micro-PET Imaging of Gliomas Model

    摘要
  • 摘要:
    目的 探讨68Ga-PSMA-617在神经胶质瘤U87MG荷瘤鼠的显像情况。
    方法 将靶向前列腺特异性膜抗原（prostate specific membrane antigen, PSMA）的新型探针DKFZ-PSMA-617进行68Ga核素标记，利用Radio-TLC对68Ga-PSMA-617的放射化学纯度进行快速质控，然后进行细胞水平实验，尾静脉注射5和40 min后对U87MG荷瘤鼠进行micro-PET显像，同时对PSMA阻滞剂ZJ-43（25 mg/kg）共注射组进行注射后40 min的图像采集。
    结果 Radio-TLC对68Ga-PSMA-617的标记率及放化纯测定可在10 min内完成，放化纯高达（99.0±1.9）%，细胞水平实验显示68Ga-PSMA-617分子探针的特异性，同时也显示U87MG细胞表面仅有较少量PSMA表达，而U87MG荷瘤鼠的micro-PET显像可见随时间延长肿瘤对PSMA靶向分子探针的放射性摄取的逐渐增高，靶与非靶比值从1.85±0.02（5 min）增长至3.62±0.175（40 min），且肿瘤对该探针的摄取可被PSMA阻滞剂ZJ-43所抑制。
    结论 68Ga-PSMA-617不仅可应用于前列腺癌的诊断，也有望应用于新生血管丰富的神经胶质瘤的诊断。

     

    Abstract:
    Objective To investigate the application of 68Ga-PSMA-617 molecular probe for micro-PET imaging of gliomas tumor model.
    Methods DKFZ-PSMA-617, an effective prostate specific membrane antigen (PSMA) targeted probes, was chosen to be the precursor to be radiolabelled with 68Ga. The radio-chemical yield of 68Ga-PSMA-617 was analyzed by Radio-TLC. Cell uptake experiments were performed on PSMA (+) LNCaP, PSMA (-) PC-3 and U87MG cells. Nude mice bearing U87MG were injected with 68Ga-PSMA-617(7.4 MBq) via the tail vein. Micro-PET imaging was performed 5 and 40 min after the injection. Blocking studies were also performed in U87MG tumor-bearing mice after 40 min of co-injection of 68Ga-PSMA-617 with the PSMA inhibitor (S)-2-(3-((S)-1-carboxy-3-methylbutyl)ureido) pentanedioic acid (ZJ-43) (25 mg/kg).
    Results The radiotracer had a good radio-chemical yield of (99.0±1.9)% quickly tested by Radio-TLC. In cell uptake experiments, the specificity of 68Ga-PSMA-617 was confirmed in PSMA (+) LNCaP cells and PSMA (-) PC-3 cells; meanwhile, it proved the low expression level of PSMA in gliomas U87MG cell line. From micro-PET imaging, U87MG xenografts tumors were visualized and it showed good tumor-to-background value from 1.85±0.02 (5 min) to 3.62±0.175 (40 min) which could be blocked by ZJ-43.
    Conclusion 68Ga-PSMA-617 has the potential to be used not only in prostate cancer but also in gliomas tumor model.

     

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