新型多肽示踪剂^(131)I-RRL肿瘤分子显像研究  

Study of Novel Peptide Probe ^(131)I-RRL for Tumor Molecular Imaging

作　　者：卢霞[1,2] 王荣福[1] 张春丽[1] 

机构地区：[1]北京大学第一医院核医学科,北京100034 [2]北京航天总医院影像中心,北京100076

出　　处：《同位素》2011年第3期177-181,共5页Journal of Isotopes

基　　金：国家自然科学基金(30870729);国家重点基础研究发展计划基金-973计划(2006CB705705);北京大学985Ⅱ期基金资助(985-2-056)

摘　　要：研究能与肿瘤血管内皮细胞特异结合的小分子多肽显像剂精氨酸-精氨酸-亮氨酸(RRL)对黑色素瘤小鼠模型的肿瘤分子显像应用价值。采用氯胺-T法对小分子多肽RRL进行131I标记,并对标记条件进行了优化;最佳标记条件为:RRL用量50μg,Na131I用量10μL(74 MBq),氯胺-T用量90μg,反应总体积100μL,振荡反应3 min。标记率>69%。用Sephadex G25柱对标记产物进行纯化,纯化后放化纯度>95%。采用绿色荧光素(FITC)标记RRL,并进行体外细胞结合实验,通过荧光信号的强弱观察RRL在不同细胞中的结合能力。体外细胞结合实验结果显示,RRL不仅能够特异性结合于肿瘤来源的血管内皮细胞,而且能够与肿瘤实质细胞结合;131I-RRL对黑色素瘤动物模型进行SPECT显像结果显示,131I-RRL能够特异性浓聚于肿瘤组织,24 h后放射性浓聚灶清晰可见。以上结果表明,小分子多肽RRL是一种很有潜力的肿瘤放射性核素分子显像与治疗的载体。To study the potential application value of Ary-Ary-Leu（RRL） specially combined with tumor derived endothelial cells in tumor molecular imaging for melanoma bearing mice,a novel peptide RRL was designed and labeled with 131I by chloramine-T method,and mice bearing melanoma tumor were injected 131I-RRL to imaging.The labeling results showed that the optimized condition were following： 50 μg RRL,10 μL（74 MBq）Na131I,90 μg chloramine-T,total reaction volume 100 μL,and reaction time 3 min,the labeling yield was over 69%.The labeling compound was purified by Sephadex G25,its radiochemical purity was 95%.In vitro binding experiments,FITC-RRL was mainly combine with tumor cells and tumor angiogenesis endothelial cells,and in the SPECT imaging,131I-RRL peptide could successfully image the tumor in nude mice bearing melanoma tumor for 24 h after injection.The results indicated that small molecular peptide RRL was a promising carrier for tumor molecular imaging and radioimmunotherapy.

关 键 词：131I标记 RRL多肽 肿瘤 分子显像 

分 类 号：R817[医药卫生—影像医学与核医学]