CAJ | 학술논문

目的：研究新型PET受体靶向显像剂18F-AlF-NOTA-PRGD2用于肿瘤显像的可行性。方法18F-AlF-NOTA-PRGD2采用18氟-氟化铝（18F-AlF）与NOTA-PRGD2在100℃下通过鳌合反应标记制备而得。荷脑胶质瘤U87MG裸鼠经尾静脉注射18F-AlF-NOTA-PRGD2后行体内放射性生物学分布和PET/CT、microPET/CT显像研究。结果18F-AlF-NOTA-PRGD2采用一步法成功标记，反应时间15~20 min，标记产率为17%~25%。体内放射性生物学研究显示该显像剂能靶向肿瘤病灶，静脉注射后1 h和2 h肿瘤摄取量分别达4.14±1.44、2.80±1.18%ID/g（t=1.910，P=0.070），肿瘤/脑比值分别达2.95±0.61、5.21±2.62（t=-1.686，P=0.167）。PET/CT和microPET/CT显像均可清楚显示该显像剂在荷瘤鼠体内的放射性分布情况，肿瘤显像清楚，体内分布良好，但microPET/CT图像质量明显优于PET/CT。结论18F-AlF-NOTA-PRGD2标记简单、易行，在荷瘤鼠体内具有优良的肿瘤靶向性，可发展成为PET肿瘤显像剂。
목적：연구신형PET수체파향현상제18F-AlF-NOTA-PRGD2용우종류현상적가행성。방법18F-AlF-NOTA-PRGD2채용18불-불화려（18F-AlF）여NOTA-PRGD2재100℃하통과오합반응표기제비이득。하뇌효질류U87MG라서경미정맥주사18F-AlF-NOTA-PRGD2후행체내방사성생물학분포화PET/CT、microPET/CT현상연구。결과18F-AlF-NOTA-PRGD2채용일보법성공표기，반응시간15~20 min，표기산솔위17%~25%。체내방사성생물학연구현시해현상제능파향종류병조，정맥주사후1 h화2 h종류섭취량분별체4.14±1.44、2.80±1.18%ID/g（t=1.910，P=0.070），종류/뇌비치분별체2.95±0.61、5.21±2.62（t=-1.686，P=0.167）。PET/CT화microPET/CT현상균가청초현시해현상제재하류서체내적방사성분포정황，종류현상청초，체내분포량호，단microPET/CT도상질량명현우우PET/CT。결론18F-AlF-NOTA-PRGD2표기간단、역행，재하류서체내구유우량적종류파향성，가발전성위PET종류현상제。
Objective To investigate the tumor targeting efficacy of 18F-AlF-NOTA-PRGD2, a novel radiotracer of Arginine-glycine-aspartic acid (RGD) peptides. Methods 18F-AlF-NOTA-PRGD2 was synthesized in one-step by conjugating NOTA-RGD2 with 18F-AlF at 100℃. The tumor targeting efficacy and in vivo biodistribution profile of 18F-AlF-NOTA-RGD2, following intravenous injection via the tail vein, were evaluated in a nude mouse model bearing subcutaneous U87MG glioblastoma xenograft by radioactivity biodistribution assessment, PET/CT and microPET/CT. Results NOTA-RGD2 was 18F-fluorinated successfully in one-step with a yield of 17%-25%within 15-20 min. Radioactivity biodistribution study confirmed the tumor-targeting ability of 18F-AlF-NOTA-PRGD2 in the tumor-bearing mice. At 1 and 2 h following injection, 18F-AlF-NOTA-PRGD2 uptake in the tumor reached 4.14 ± 1.44 and 2.80 ± 1.18%ID/g (t=1.910, P=0.070) with tumor/brain ratios of 2.95 ± 0.61 and 5.21 ± 2.62, respectively (t=-1.686, P=0.167). Both PET/CT and microPET/CT were capable of showing the radioactivity biodistribution of 18F-AlF-NOTA-PRGD2 in the mouse model and clearly displayed the tumor, but microPET/CT showed a much better image quality. Conclusion 18F- AlF- NOTA- PRGD2 prepared by one- step radiosynthesis can selectively target to the tumor, demonstrating its potential as a good radiotracer for tumor imaging.