CAJ | 학술논문

目的应用多功能放射性药物标记模块Explora GN联合液相分离模块Explora LC 制备高纯度的16α-[18F]氟-17β-雌二醇(18F-FES).方法基于Explora GN多功能合成模块和Explora LC液相色谱分离模块,同时结合自制的固相萃取装置,采用"一锅法"完成18F-FES的合成和分离.用分析型HPLC测18F-FES的放化纯.进行18F-FES与ER阳性细胞(MCF-7细胞)的饱和结合实验.结果该方法的总合成时间(包括HPLC分离和赋型)为60 min,放射化学产率为45%(衰减校正之后),放化纯>98%,没有明显的化学杂质.MCF-7细胞和18F-FES结合表现为受体与配体的可饱和性实验特性,Kd和Bmax分别为(2.922±0.619) nmol/L和(4.193±0.360) nmol/L.结论应用Explora GN/LC双模块成功地制备了高化学纯度和高放化纯的18F-FES;18F-FES具有与ER结合的特性,可为乳腺癌ER PET/CT显像提供安全、有效的特异性显像剂.
목적 응용다공능방사성약물표기모괴Explora GN연합액상분리모괴Explora LC 제비고순도적16α-[18F]불-17β-자이순(18F-FES).방법 기우Explora GN다공능합성모괴화Explora LC액상색보분리모괴,동시결합자제적고상췌취장치,채용"일과법"완성18F-FES적합성화분리.용분석형HPLC측18F-FES적방화순.진행18F-FES여ER양성세포(MCF-7세포)적포화결합실험.결과 해방법적총합성시간(포괄HPLC분리화부형)위60 min,방사화학산솔위45%(쇠감교정지후),방화순>98%,몰유명현적화학잡질.MCF-7세포화18F-FES결합표현위수체여배체적가포화성실험특성,Kd화Bmax분별위(2.922±0.619) nmol/L화(4.193±0.360) nmol/L.결론 응용Explora GN/LC쌍모괴성공지제비료고화학순도화고방화순적18F-FES;18F-FES구유여ER결합적특성,가위유선암ER PET/CT현상제공안전、유효적특이성현상제.
Objective To synthesize 16α-[18F]fluoro-17β-estrogen(18F-FES) with high chemical and radiochemical purity using multifunctional radiolabeling module of Explora GN and separation module of Explora LC (Explora GN/LC dual module). Methods Explora GN/LC dual module and "one-pot" radiochemical process were applied for fully automated synthesis and separation of 18F-FES. The radiochemical purity of 18F-FES was analyzed by HPLC. The saturation binding test of 18F-FES with ER (ER-positive MCF-7 cell line) was applied to examine the biological activity of 18F-FES. Results 18F-FES synthesis procedure took 60 min, with radiochemical yield about 45% and radiochemical purity higher than 98%. The Kd and Bmax of MCF-7 cells with 18F-FES were (2.922±0.619) nmol/L and (4.193±0.360) nmol/L respectively. Conclusions 18F-FES can be automatically synthesized by Explora GN/LC dual module with high chemical purity and radiochemical purity. It would be a potential PET tracer to be used in estrogen-related molecular imaging.