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

• Main Authors: HAN Xuedi, LIU Fei, GUO Xiaoyi, XU Xiaoxia, XIE Qinghua, LIU Teli, ZHU Hua, YANG Zhi
• Format: Article
• Language: zho
• Published: Magazine House of Cancer Research on Prevention and Treatment 2018-07-01
• Series: Zhongliu Fangzhi Yanjiu
• Subjects: prostate specific membrane antigen; neo-vasculature; pet; glioma; gallium-68
• Online Access: http://html.rhhz.net/ZLFZYJ/html/8578.2018.17.0405.htm

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.