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学科主题: 临床医学
题名:
Synthesis and Biodistribution of a New 99mTc-oxo Complex with Deoxyglucose Dithiocarbamate for Tumor Imaging
作者: 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
发表日期: 2012-03-01
DOI: 10.1111/j.1747-0285.2011.01280.x
卷: 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
所属项目编号: 21171024
项目资助者: National Natural Science Foundation of China ; Fundamental Research Funds for the Central Universities
WOS记录号: WOS:000299253200002
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/58279
Appears in Collections:北京大学第三临床医学院_核医学科_期刊论文

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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

Recommended Citation:
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.
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