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学科主题临床医学
Synthesis and Biodistribution of a New 99mTc-oxo Complex with Deoxyglucose Dithiocarbamate for Tumor Imaging
Lin, Xiao1; Jin, Zhonghui2; Ren, Jialei1; Pang, Yan1; Zhang, Weifang2; Huo, Jinfeng1; Wang, Xuebin1; Zhang, Junbo1; Zhang, Yanyan2
关键词99mTc-oxo complex biodistribution deoxyglucose dithiocarbamate ligand-exchange tumor
刊名CHEMICAL BIOLOGY & DRUG DESIGN
2012-03-01
DOI10.1111/j.1747-0285.2011.01280.x
79期:3页:239-245
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology ; Chemistry, Medicinal
研究领域[WOS]Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
关键词[WOS]BIOLOGICAL EVALUATION ; RADIOPHARMACEUTICALS ; AGENT
英文摘要

The deoxyglucose dithiocarbamate (DGDTC) was radiolabeled with 99mTc(V)-glucoheptonate (GH), for the potential use as radiopharmaceuticals for tumor imaging. For labeling, 99mTcO-DGDTC was prepared by ligand-exchange reaction with 99mTc-GH. The radiochemical purity of the 99mTcO-DGDTC complex was over 90% by thin-layer chromatography and high-performance liquid chromatography, without any notable decomposition at room temperature over a period of 6 h. Its partition coefficient indicated that it was a hydrophilic complex. The ligand-exchange reaction occured at neutral condition and under 100 degrees C for 15 min to achieve high radiochemical purity. In vitro cell studies showed there was an increase in the uptake of 99mTcO-DGDTC as a function of incubation time and the cellular uptake of 99mTcO-DGDTC was possibly mediated by way of a d-glucose mechanism. The biodistribution of 99mTcO-DGDTC in mice bearing S 180 tumor showed that the complex accumulated in the tumor with good uptake and excellent retention. As compared with other reported 99mTc radiolabeled glucose derivatives, 99mTcO-DGDTC showed the highest tumor uptake and good tumor/muscle ratios. The tumor/muscle ratio of 99mTcO-DGDTC uptake was higher than that of [18F] FDG uptake. Single photon emission computed tomography (SPECT) image studies showed there was a visible accumulation in tumor sites, suggesting 99mTcO-DGDTC would be a promising candidate for tumor imaging.

语种英语
WOS记录号WOS:000299253200002
项目编号21171024
资助机构National Natural Science Foundation of China ; Fundamental Research Funds for the Central Universities
引用统计
被引频次:19[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/400002259/58279
专题北京大学第三临床医学院_核医学科
作者单位1.Beijing Normal Univ, Coll Chem, Minist Educ, Key Lab Radiopharmaceut, Beijing 100875, Peoples R China
2.Peking Univ, Dept Nucl Med, Hosp 3, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Lin, Xiao,Jin, Zhonghui,Ren, Jialei,et al. Synthesis and Biodistribution of a New 99mTc-oxo Complex with Deoxyglucose Dithiocarbamate for Tumor Imaging[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2012,79(3):239-245.
APA Lin, Xiao.,Jin, Zhonghui.,Ren, Jialei.,Pang, Yan.,Zhang, Weifang.,...&Zhang, Yanyan.(2012).Synthesis and Biodistribution of a New 99mTc-oxo Complex with Deoxyglucose Dithiocarbamate for Tumor Imaging.CHEMICAL BIOLOGY & DRUG DESIGN,79(3),239-245.
MLA Lin, Xiao,et al."Synthesis and Biodistribution of a New 99mTc-oxo Complex with Deoxyglucose Dithiocarbamate for Tumor Imaging".CHEMICAL BIOLOGY & DRUG DESIGN 79.3(2012):239-245.
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