^(99)Tc^m标记NGR及其在荷人HePG2肝癌裸鼠体内的生物分布及SPECT显像  

Biodistribution and SPECT Imaging of ^(99)Tc^m Labeling NGR Peptide in Nude Mice Bearing Human HePG2 Hepatoma

作　　者：马温惠[1] 汪静[1] 杨卫东[1] 李桂玉[1] 马晓伟[1] 王喆[1] 

机构地区：[1]第四军医大学西京医院核医学科,陕西西安710032

出　　处：《同位素》2012年第1期27-32,共6页Journal of Isotopes

基　　金：国家自然科学基金资助项目(30970846);国家重点基础研究发展计划(2011CB707704)

摘　　要：用99 Tcm标记了含有天冬酰胺-甘氨酸-精氨酸(Asn-Gly-Arg)序列的血管靶向性短肽NGR,评价了标记物99 Tcm-NGR的放化性质以及在荷HePG2肝癌模型裸鼠体内的生物分布和SPECT显像。标记结果显示,99 Tcm-NGR的标记率>90%,放化纯度>95%。荷瘤裸鼠体内生物分布结果显示,99 Tcm-NGR在肾脏和肝脏的摄取率较高,注射后1h肿瘤摄取达(2.52±0.62)%ID/g,最高达(7.26±2.71)%ID/g,12h仍然达(3.93±1.93)%ID/g,但在竞争性抑制组中摄取率为(1.29±0.85)%ID/g。荷瘤裸鼠的SPECT显像结果显示,除肿瘤外,其他组织器官的放射性摄取随时间延长逐渐降低,肿瘤与肌肉组织的放射性攝取比(T/NT)4h时最高,可达3.25。注射后1h肿瘤可见,12h时最为清晰。以上结果提示,99 Tcm-NGR易于制备,具有良好的靶向性,在肿瘤的诊疗中具有良好的研究前景。A peptide containing the Asn-Gly-Arg（NGR）sequence was radiolabeled by 99Tcm and its radiochemical characteristics,biodistribution and SPECT imaging in nude mice bearing human HePG2 hepatoma were evaluated.99Tcm-NGR was prepared directly with a labeling yield higher than 90%,and the radiochemical purity（RCP） higher than 95%.Nude mice bearing human HePG2 hepatoma were randomly divided into 6 groups with 3 mice in each group.The control group mice were blocked by injecting 100 μg unlabeled NGR 0.5 h before 99Tcm-NGR injection.The mice were sacrificed at 1、2、4、8、12 h after caudal intravenous injection of 7.4 MBq 99Tcm-NGR.The uptakes of kidney and liver were very high.Tumor uptake was（2.52±0.62）%ID/g at 1 h,with the highest uptake of（7.26±2.71）%ID/g.At 12 h,the uptake was still（3.93±1.93）%ID/g.In comparison,the uptake of the blocked control group was（1.29±0.85）%ID/g.The SPECT static images of 3 mice and the tumor/muscle（T/NT） value were obtained.The highest T/NT value was 3.25 at 4 h.The xenografted tumor became visible at 1h and the clearest image of the tumor was observed at 12 h.Results from this work shows that 99Tcm-NGR can be efficiently prepared,can favorably target tumor angiogenesis,and should be a potential probe in tumor therapy.

关 键 词：99Tcm NGR 肿瘤 SPECT显像 

分 类 号：TL92[核科学技术—核燃料循环与材料] R817[医药卫生—影像医学与核医学]