^(125)I标记的羊抗人IgG多克隆抗体在荷人结肠癌裸鼠体内的生物分布及γ显像  

Biodistribution and γ Imaging of ^(125)I-labeled Goat Anti-human IgG Polyclonal Antibody in Nude Mice Bearing Human Colon Cancer Xenografts

作　　者：贺巍巍[1] 刘昭飞[2] 贾兵[2] 邱晓彦[3] 王凡[2] 

机构地区：[1]北京大学药学院天然药物与仿生药物国家重点实验室,北京100083 [2]北京大学医学同位素研究中心,北京100083 [3]北京大学人类疾病基因研究中心,北京100083

出　　处：《同位素》2008年第2期77-81,共5页Journal of Isotopes

基　　金：国家"863"资助项目(2007AA02Z467)

摘　　要：采用Iodogen法对羊抗人IgG多克隆抗体(GAHG)进行125I标记,并观察了125I-GAHG在荷HT-29人结肠癌裸鼠体内的生物分布和γ显像,以探讨肿瘤细胞分泌的IgG作为靶点进行肿瘤放射免疫显像和治疗的可能性。结果显示,125I-GAHG具有良好的体外稳定性,其血液清除符合二室模型,T1/2α和T1/2β分别为1.19 h和43.99 h。尾静脉给药后,与125I标记的正常羊IgG(125I-IgG)对照相比,125I-GAHG具有更加明显的肿瘤摄取。瘤体内给药的实验结果显示,125I-GAHG在肿瘤部位具有良好的滞留。在静脉注射后72 h,肿瘤摄取达到最大,为6.71±2.19%ID/g。靶与非靶组织的放射性摄取比(T/NT)随着时间延长逐渐增大。上述结果提示,125I-GAHG具有肿瘤特异性摄取,这为以肿瘤分泌的IgG为靶点的肿瘤放射免疫显像和靶向治疗提供了新思路。The possibility of IgG secreted from tumor cells as a target for radioimmunoimaging and targeted therapy of cancers were investigated. Goat anti-human IgG polyclonal antibody （GAHG） was radioiodinated using Iodogen method, and the in vitro stability and pharmacokinetics were evaluated. The biodistribution and 7 imaging of ^125I-GAHG were performed in nude mice bearing HT-29 human colon cancer xenografts. ^125I-GAHG showed good in vitro stability, and its blood clearance was defined as a two-compartment model, with T1/2α and T1/2β were 1.19 h and 43.99 h, respectively. The tumor uptake of ^125I-GAHG was higher than that of ^125I-labeled normal goat IgG control （^125 I-GIgG）. ^125I-GAHG showed good tumor retention when injecting via intra-tumor. In the biodistribution study, the highest tumor uptake of ^125I-GAHG was 6.71±2.19 %ID/g at 72 h postinjection and the T/NT increased along with the postinjection time. The results show that ^125I-GAHG have good tumor-specific uptake which may provide a novel idea for radioimmunoimaging and targeted therapy of cancers.

关 键 词：IGG ^125I 肿瘤显像 生物分布 

分 类 号：TQ463.7[化学工程—制药化工] R817-33[医药卫生—影像医学与核医学]