CAJ | 학술논문

目的应用国产多功能18F标记模块制备4-[18F]氟-3-三氟甲基苯甲酰基-谷氨酸-(RGD -苯丙氨酸-赖氨酸)环肽二聚体(4-18 F-TFMB-E[c(RGDfk)2]),并用micro PET观察其在肿瘤模型鼠内的生物分布.方法基于PET-MF-2V-IT-I多功能合成模块,采用“一锅法”完成4-18F-TFMB-E[ c(RGDfk)2]的制备和纯化.荷人胰腺癌BxPC-3裸鼠给药后行micro PET活体显像.结果 4-18 F-TFMB-E[ c(RGDfk)2]放化产率为(27.4±2.3)％(衰减校正后),总合成时间为30 min,无需HPLC法分离,放化纯＞98％.荷人胰腺癌BxPC-3裸鼠注射4-18 F-TFMB-E[c(RGDfk)2]后30、60和120 min后肿瘤摄取值(％ID/g)分别为4.03±0.32、3.31±0.20和2.72±0.17；注射后30 min肿瘤与对侧肌肉摄取值比值大于6(对侧肌肉摄取值为0.47 ±0.12).4-18F-TFMB-E[c (RGDfk)2]主要经肝、肠排泄.结论 4-18F-TFMB-E[ c(RGDfk)2]自动化合成速度快、效率高,胰腺癌肿瘤模型显影清晰.
목적 응용국산다공능18F표기모괴제비4-[18F]불-3-삼불갑기분갑선기-곡안산-(RGD -분병안산-뢰안산)배태이취체(4-18 F-TFMB-E[c(RGDfk)2]),병용micro PET관찰기재종류모형서내적생물분포.방법 기우PET-MF-2V-IT-I다공능합성모괴,채용“일과법”완성4-18F-TFMB-E[ c(RGDfk)2]적제비화순화.하인이선암BxPC-3라서급약후행micro PET활체현상.결과 4-18 F-TFMB-E[ c(RGDfk)2]방화산솔위(27.4±2.3)％(쇠감교정후),총합성시간위30 min,무수HPLC법분리,방화순＞98％.하인이선암BxPC-3라서주사4-18 F-TFMB-E[c(RGDfk)2]후30、60화120 min후종류섭취치(％ID/g)분별위4.03±0.32、3.31±0.20화2.72±0.17；주사후30 min종류여대측기육섭취치비치대우6(대측기육섭취치위0.47 ±0.12).4-18F-TFMB-E[c (RGDfk)2]주요경간、장배설.결론 4-18F-TFMB-E[ c(RGDfk)2]자동화합성속도쾌、효솔고,이선암종류모형현영청석.
Objective To prepare4-[18F]fluoro-3-trifluoromethylbenzoyl-E[c(RGDfk)2] (4-18F-TFMB-E[ c(RGDfk) 2 ] ) using a domestic multifunctional 18 F radiolabeling module and study the biodistribution of 4-18F-TFMB-E[c(RGDfk)2] in tumor-bearing mice by micro PET.Methods PET-MF-2V-IT-I multifunctional synthesis module and "one-pot" radio-chemical procedure were applied for the synthesis and purification of 4-18F-TFMB-E[ c(RGDfk)2 ].Nude mice bearing human pancreatic cancer BxPC-3 cells were imaged by micro PET after intravenous injection of 4-18 F-TFMB-E [ c (RGDfk)2 ] for biodistribution study.Results The total synthesis duration was 30 min.The radiochemical yield of 4-18F-TFMB-E[ c(RGDfk)2 ] was (27.4 ± 2.3)％ (decay corrected) and the radiochemical purity was more than 98％ without HPLC purification.Tumor uptake of 4-18 F-TFMB-E [ c (RGDfk) 2 ] was (4.03 ± 0.32),(3.31 ± 0.20) and (2.72 ± 0.17) ％ ID/g at 30,60 and 120 min postinjection,respectively.The tumor/muscle uptake ratio was greater than 6 (0.47 ±0.12,％ ID/g in muscle) at 30 min postinjection.The predominant excretion pathway was via liver and intestine.The uptake of 4-18 F-TFMB-E [ c (RGDfk) 2 ] in liver and intestine was 2.08 ±0.24 and 1.62 ± 0.24,respectively.Conclusions 4-18 F-TFMB-E [ c (RGDfk) 2 ] can be automatically and quickly synthesized with a high radiochemical yield and purity.The prepared 4-18F-TFMB-E[ c(RGDfk) 2 ]might be a potential agent for pancreatic tumor imaging.