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学科主题临床医学
A Novel Tc-99m-Labeled Molecular Probe for Tumor Angiogenesis Imaging in Hepatoma Xenografts Model: A Pilot Study
Zhao, Qian; Yan, Ping; Wang, Rong Fu; Zhang, Chun Li; Li, Ling; Yin, Lei
刊名PLOS ONE
2013-04-03
DOI10.1371/journal.pone.0061043
8期:4
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Multidisciplinary Sciences
资助者Research Fund Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, Department of Chemistry, Beijing Normal University, Beijing, China ; Natural Science Foundation of China ; Ministry of Science and Technology of China ; Research Fund for the Medicine and Engineering of Peking University ; Research Fund Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, Department of Chemistry, Beijing Normal University, Beijing, China ; Natural Science Foundation of China ; Ministry of Science and Technology of China ; Research Fund for the Medicine and Engineering of Peking University
研究领域[WOS]Science & Technology - Other Topics
关键词[WOS]ARGININE-ARGININE-LEUCINE ; PEPTIDE ; BINDING ; BIODISTRIBUTION ; CARCINOMA ; ANTIBODY ; CANCER
英文摘要

Introduction: Visualization of tumor angiogenesis using radionuclide targeting provides important diagnostic information. In previous study, we proved that an arginine-arginine-leucine (RRL) peptide should be a tumor endothelial cell specific binding sequence. The overall aim of this study was to evaluate whether Tc-99m-radiolabeled RRL could be noninvasively used for imaging of malignant tumors in vivo, and act as a new molecular probe targeting tumor angiogenesis.

Methods: The RRL peptide was designed and radiosynthesized with Tc-99m by a one-step method. The radiolabeling efficiency and radiochemical purity were then characterized in vitro. Tc-99m-RRL was injected intravenously in HepG2 xenograft-bearing BALB/c nude mice. Biodistribution and in vivo imaging were performed periodically. The relationship between tumor size and %ID uptake of Tc-99m-RRL was also explored.

Results: The labeling efficiencies of Tc-99m-RRL reached 76.9%+/- 64.5% (n = 6) within 30-60 min at room temperature, and the radiochemical purity exceeded 96% after purification. In vitro stability experiment revealed the radiolabeled peptide was stable. Biodistribution data showed that Tc-99m-RRL rapidly cleared from the blood and predominantly accumulated in the kidneys and tumor. The specific uptake of Tc-99m-RRL in tumor was significantly higher than that of unlabeled RRL blocking and free pertechnetate control test after injection (p<0.05). The ratio of the tumor-to-muscle exceeded 6.5, tumor-to-liver reached 1.98 and tumor-to-blood reached 1.95. In planar gamma imaging study, the tumors were imaged clearly at 2-6 h after injection of Tc-99m-RRL, whereas the tumor was not imaged clearly in blocking group. The tumor-to-muscle ratio of images with Tc-99m-RRL was comparable with that of F-18-FDG PET images. Immunohistochemical analysis verified the excessive vasculature of tumor. There was a linear relationship between the tumor size and uptake of Tc-99m-RRL with R-2 = 0.821.

Conclusion: Tc-99m-RRL can be used as a potential candidate for visualization of tumor angiogenesis in malignant carcinomas.

语种英语
所属项目编号120201 ; NSFC 30870729 ; 81071183 ; 2011YQ030114 ; 2011YQ03011409 ; BMU20120297
资助者Research Fund Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, Department of Chemistry, Beijing Normal University, Beijing, China ; Natural Science Foundation of China ; Ministry of Science and Technology of China ; Research Fund for the Medicine and Engineering of Peking University ; Research Fund Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, Department of Chemistry, Beijing Normal University, Beijing, China ; Natural Science Foundation of China ; Ministry of Science and Technology of China ; Research Fund for the Medicine and Engineering of Peking University
WOS记录号WOS:000318840100112
引用统计
被引频次:3[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/50229
专题北京大学第一临床医学院_核医学科
作者单位Peking Univ, Hosp 1, Dept Nucl Med, Beijing 100871, Peoples R China
推荐引用方式
GB/T 7714
Zhao, Qian,Yan, Ping,Wang, Rong Fu,et al. A Novel Tc-99m-Labeled Molecular Probe for Tumor Angiogenesis Imaging in Hepatoma Xenografts Model: A Pilot Study[J]. PLOS ONE,2013,8(4).
APA Zhao, Qian,Yan, Ping,Wang, Rong Fu,Zhang, Chun Li,Li, Ling,&Yin, Lei.(2013).A Novel Tc-99m-Labeled Molecular Probe for Tumor Angiogenesis Imaging in Hepatoma Xenografts Model: A Pilot Study.PLOS ONE,8(4).
MLA Zhao, Qian,et al."A Novel Tc-99m-Labeled Molecular Probe for Tumor Angiogenesis Imaging in Hepatoma Xenografts Model: A Pilot Study".PLOS ONE 8.4(2013).
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