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Radio-labelling and Micro-PET Study of Cu-64 Labelled PnAO-1-(2-nitroimidazole) for Hypoxia Imaging
Luo Zheng1; Zhu Hua1; Lin Xinfeng1; Hong Ye1; Xiao Shaowen2; Zhang Qiang3; Chu Taiwei3; Yang Zhi1
关键词Nitroimidazole Cu-64 Positron emission tomography Hypoxia imaging
刊名CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE
2015-01-10
DOI10.7503/cjcu20140438
36期:1页:87-92
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Multidisciplinary
研究领域[WOS]Chemistry
关键词[WOS]AMINE OXIME COMPLEXES ; BIOLOGICAL EVALUATION ; TUMOR HYPOXIA ; IN-VITRO ; CANCER ; BISNITROIMIDAZOLE ; MARKERS
英文摘要

Monitoring hypoxia is very important for tumor treatment, the ideal hypoxia imaging agents should have a relatively long half-life and specific to hypoxic cells. However, such an ideal imaging agent has not been developed until now. In order to develop an ideal imaging agent for monitoring hypoxia, nitroimidazole imaging agent PnAO-1-(2-nitroimidazole) [BMS181321] was synthesized and radiolabeled with Cu-64 for Cu-64-BMS181321. The basic experimental process is as follows; the BMS181321 dissolved in sodium acetate buffer (pH =5. 5) was added to the eluent of (CuCl2)-Cu-64, and the solution was stirred and placed at room temperature for 10 min. The labelling efficiency and radiochemical purity of Cu-64-BMS181321 were all over 99%, determined by radio-HPLC. The Cu-64-BMS181321 was stable in physiological saline for more than 15 h, which was a meaningful characteristic for clinical application. After quality control, 21. 8 MBq of Cu-64-BMS181321 was injected into human pancreatic cancer xenograft mouse models via tale vein. Positron emission tomography (PET) images were taken at 4 and 8 h after the injection. PET imaging in human tumor models was excellent compared with other PET hypoxia imaging agents. In brief, the research results suggest that Cu-64-BMS181321 is potential for PET hypoxia imaging in clinical and should be further evaluated in clinic trial.

语种中文
WOS记录号WOS:000348750100012
项目编号81071198 ; 81172083 ; 81371592 ; 7132040
资助机构National Natural Science Foundation of China ; Beijing Municipal Natural Science Foundation, China
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/400002259/58285
专题北京大学临床肿瘤学院_核医学科
北京大学第一临床医学院_肾脏内科
北京大学临床肿瘤学院_肿瘤放疗科
作者单位1.Peking Univ, Canc Hosp & Inst, Key Lab Carcinogenesis & Translat Res, Dept Nucl Med,Minist Educ, Beijing 100142, Peoples R China
2.Peking Univ, Canc Hosp & Inst, Dept Radiat Oncol, Beijing 100142, Peoples R China
3.Peking Univ, Coll Chem & Mol Engn, Beijing 100871, Peoples R China
推荐引用方式
GB/T 7714
Luo Zheng,Zhu Hua,Lin Xinfeng,et al. Radio-labelling and Micro-PET Study of Cu-64 Labelled PnAO-1-(2-nitroimidazole) for Hypoxia Imaging[J]. CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE,2015,36(1):87-92.
APA Luo Zheng.,Zhu Hua.,Lin Xinfeng.,Hong Ye.,Xiao Shaowen.,...&Yang Zhi.(2015).Radio-labelling and Micro-PET Study of Cu-64 Labelled PnAO-1-(2-nitroimidazole) for Hypoxia Imaging.CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE,36(1),87-92.
MLA Luo Zheng,et al."Radio-labelling and Micro-PET Study of Cu-64 Labelled PnAO-1-(2-nitroimidazole) for Hypoxia Imaging".CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE 36.1(2015):87-92.
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