叶酸修饰PAMAM树状大分子的合成及^188Re标记  

Synthesis and radiolabelling of ^(188)Re labeled dendrimer PAMAM-folic acid conjugate

作　　者：崔巍[1,2] 张元庆[1,2] 许晓平[1,2] 沈玉梅[1,3] 

机构地区：[1]中国科学院上海应用物理研究所放射性药物中心,上海201800 [2]中国科学院研究生院,北京100049 [3]上海交通大学系统生物医学研究院,系统生物医学教育部重点实验室,上海200240

出　　处：《核技术》2011年第5期386-390,共5页Nuclear Techniques

基　　金：国家自然科学基金项目(8107125)资助

摘　　要：叶酸受体在多种肿瘤细胞中过表达是癌症治疗中一种可能的靶向药物结合位点。我们将五代PAMAM树状大分子用叶酸和1B4M-DTPA修饰,然后用^(188)Re进行放射性标记。化合物的标记产率为67.5%,分离后的放射化学纯度大于95%,并表现出良好的体外稳定性,为该化合物在叶酸受体靶向肿瘤治疗应用中奠定了基础。Folic acid receptor （FR） was usually overexpressed in many cancer cells and was considered as potential target for targeted therapy agent. We decorated dendrimer polyamidoamine generation five-folic with acid and 1B4M-DTPA and then radiolabelled with 188Re. Thes in vitro stability was evaluated. The labeling yield of the G5-FA-DTPA-188Re was 67.5%, with a radiochemical purity of over 95%. The conjugate also showed high in vitro stability. Further modifications on the dendrimer folic acid conjugate and biological evaluation is in progress and will be reported in due course.

关 键 词：树状大分子 ^188RE 放射性标记 叶酸 

分 类 号：O625.3[理学—有机化学]