抗人肝癌单抗Hepama-1间接碘标记及其生物分布  

Indirect radioiodination of Hepama-1 with N-Succinimidyl 3-iodo[^(125)I]benzoate and its biodistribution in normal mice

作　　者：刘振锋[1] 汪勇先[2] 周伟[2] 尹端沚[2] 

机构地区：[1]浙江大学医学院附属第一医院核医学科,杭州310003 [2]中国科学院上海应用物理研究所,上海201800

出　　处：《核技术》2007年第10期850-854,共5页Nuclear Techniques

基　　金：中国科学院创新工程重大项目(KJCXI-SW-08);国家自然科学基金项目(10405034)资助

摘　　要：研究能有效降低体内脱碘的抗体的标记方法。碘标记N–琥珀酰亚胺3–(三正丁基锡)苯甲酸酯(ATE)前体,得到N–琥珀酰亚胺3–碘[125I]苯甲酸酯(S125IB),与Hepama-1进行偶联后,对小鼠进行了生物体内分布实验,探索标记最佳条件以及测定标记物的稳定性和生物活性。结果显示ATE用N–氯代琥珀酰亚胺酯(NCS)法进行125I标记,标记率大于98%,SIB和人Hepama-1的偶联率可达90%,稳定性、生物活性良好。生物分布结果表明:与直接标记相比较,间接标记的Hepama-1大大地提高了体内稳定性,减少甲状腺的放射性摄取,血液中放射性浓度是直接标记Hepama-1的二倍,有利于单抗药物在靶位置的浓集。The work is aimed at finding an effective way to acquire radiolabeled antibody with excellent in vivo stability. N-Succinimidyl 3-iodo[^1251]benzoate （S^125IB） was obtained from radioiodination of N-Succinimidyl 3-（tri-n-butylstannyl） benzoate （ATE）. and S^1251B was conjugated to Hepama-1. The radioiodination condition was optimized and the stability and biological activity in vitro of ^125IBA-Hepama-1 was evaluated. Animal biodistribution studies were carried out. The labeling ratio of radioiodination of ATE using N-chlorosuccinimide （NCS） was more than 98%, and the conjugation efficiency of S^125IB and Hepama-1 was up to 90%, with good stability and biological activity. The localization of radioactivity observed in thyroids of mice decreased obviously. The results show that indirect radiolabeling procedure with ATE is an excellent and efficient way for radiohalogenation of Hepama-1 and other proteins or peptides.

关 键 词：碘标记 Hepama-1 N-琥珀酰亚胺3-碘【^125I】苯甲酸酯(S^125IB) 

分 类 号：R142.3[医药卫生—公共卫生与预防医学]