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Synthesis and Biodistribution of a Novel (TcN)-Tc-99m Complex of Norfloxacin Dithiocarbamate as a Potential Agent for Bacterial Infection Imaging
Zhang, Shijian1; Zhang, Weifang2; Wang, Yue1; Jin, Zhonghui2; Wang, Xuebin1; Zhang, Junbo1; Zhang, Yanyan2
刊名BIOCONJUGATE CHEMISTRY
2011-03-01
DOI10.1021/bc100357w
22期:3页:369-375
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemical Research Methods ; Biochemistry & Molecular Biology ; Chemistry, Multidisciplinary ; Chemistry, Organic
研究领域[WOS]Biochemistry & Molecular Biology ; Chemistry
关键词[WOS]TC-99M-CIPROFLOXACIN ; BOND
英文摘要

Achieving a Tc-99m-labeled fluoroquinolone derivative as a single photon emission computed tomography (SPECT) tracer is considered to be of great interest. The norfloxacin dithiocarbamate (NFXDTC) was synthesized and radiolabeled with a [(TcN)-Tc-99m](2+) intermediate to form the (TcN)-Tc-99m-NFXDTC complex in high yield. The radiochemical purity of (TcN)-Tc-99m-NFXDTC was over 90%, as measured by thin layer chromatography (TLC) and high performance liquid chromatography (HPLC), without any notable decomposition at room temperature over a period of 6 h. The partition coefficient and electrophoresis results indicated that (TcN)-Tc-99m-NFXDTC was lipophilic and neutral. The bacterial binding assay studies showed tht (TcN)-Tc-99m-NFXDTC had a good binding affinity. Biodistribution results in bacterial infected mice showed that (TcN)-Tc-99m-NFXDTC had a higher uptake at the sites of infection and better abscess/blood and abscess/muscle ratios than those of Tc-99m-ciprofloxacin and (TcN)-Tc-99m-CPFXDTC (CPFXDTC = ciprofloxacin dithiocarbamate). The biodistribution results of (TcN)-Tc-99m-NFXDTC in bacterially infected mice and in mice with turpentine-induced abscesses indicated that (TcN)-Tc-99m-NFXDTC was suited to be a bacteria-specific infection imaging agent. Single photon emission computed tomography (SPECT) image studies showed there was a visible accumulation in infection sites, suggesting that it would be a promising candidate for bacterial infection imaging.

语种英语
WOS记录号WOS:000288401400008
项目编号20771018
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:20[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/400002259/56074
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, Key Lab Radiopharmaceut, Minist Educ, Coll Chem, Beijing 100875, Peoples R China
2.Peking Univ, Hosp 3, Dept Nucl Med, Beijing, Peoples R China
推荐引用方式
GB/T 7714
Zhang, Shijian,Zhang, Weifang,Wang, Yue,et al. Synthesis and Biodistribution of a Novel (TcN)-Tc-99m Complex of Norfloxacin Dithiocarbamate as a Potential Agent for Bacterial Infection Imaging[J]. BIOCONJUGATE CHEMISTRY,2011,22(3):369-375.
APA Zhang, Shijian.,Zhang, Weifang.,Wang, Yue.,Jin, Zhonghui.,Wang, Xuebin.,...&Zhang, Yanyan.(2011).Synthesis and Biodistribution of a Novel (TcN)-Tc-99m Complex of Norfloxacin Dithiocarbamate as a Potential Agent for Bacterial Infection Imaging.BIOCONJUGATE CHEMISTRY,22(3),369-375.
MLA Zhang, Shijian,et al."Synthesis and Biodistribution of a Novel (TcN)-Tc-99m Complex of Norfloxacin Dithiocarbamate as a Potential Agent for Bacterial Infection Imaging".BIOCONJUGATE CHEMISTRY 22.3(2011):369-375.
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