特异性靶向高转移骨肉瘤的长循环型PET探针的合成及显像  

Synthesis and imaging of long-circulating PET probes specifically targeting highly metastatic osteosarcoma

作　　者：李业森[1] LI Yesen(Department of Nuclear Medicine,the First Affliated Hospital of Xiamen University,Xiamen,Fujian 361003,China)

机构地区：[1]厦门大学附属第一医院核医学科,厦门361003

出　　处：《福建医药杂志》2023年第6期127-129,共3页Fujian Medical Journal

摘　　要：目的 研究[^(64)Cu]Cu-DOTA-EB-TMTP1对143B骨肉瘤荷瘤小鼠模型的诊断效果。方法 多肽TMTP1(NVVRQ)对高转移性细胞有很好的靶向性,本研究利用^(64)Cu标记DOTA-EB-TMTP1合成[^(64)Cu]Cu-DOTA-EB-TMTP1,然后对143B骨肉瘤肝癌荷瘤小鼠进行microPET/CT显像,研究其对肿瘤的诊断效果。结果 [^(64)Cu]Cu-DOTA-EB-TMTP1的放射性标记产率为(87.3±5.2)%,放化纯度大于95.0%。实验证明经过伊文思蓝(Evans Blue)修饰后的TMTP1,具有更高的肿瘤摄取和更长的血液半衰期,8 h肿瘤摄取值可达(6.50±0.88)%ID/g。结论 对于骨肉瘤的诊断来说,[^(64)Cu]Cu-DOTA-EB-TMTP1可能是更好的PET探针,更有利于肿瘤的诊疗一体化转化应用。Objective To assess the diagnostic effectiveness of[^(64)Cu]Cu-DOTA-EB-TMTP1 in a mouse model of 143B osteosarcoma.Methods Polypeptide TMTP1(NVVRQ)had good targeting effect on highly metastatic cells.[^(64)Cu]Cu-DOTA-EB-TMTP1 was synthesized and subsequently used for microPET/CT imaging in a mouse model of 143B osteosarcoma to investigate its diagnostic performance.Results The radiolabeling yield of[^(64)Cu]Cu-DOTA-EB-TMTP1 was(87.3±5.2)%,and the radiochemical purity exceeded 95.0%.The results demonstrated that TMTP1,modified with Evans Blue,exhibited increased tumor uptake and a longer blood half-life.Tumor uptake values reached(6.50±0.88)%ID/g at eight hours.Conclusion[^(64)Cu]Cu-DOTA-EB-TMTP1 may represent a superior PET probe for the diagnosis of osteosarcoma,facilitating the integration of diagnosis and therapy for this condition.

关 键 词：PET 骨肉瘤 [^(64)Cu]Cu-DOTA-EB-TMTP1 ^(64)Cu标记 

分 类 号：R814[医药卫生—影像医学与核医学]