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学科主题: 临床医学
题名:
Synthesis and Biodistribution of a Novel (TcN)-Tc-99m Complex of Norfloxacin Dithiocarbamate as a Potential Agent for Bacterial Infection Imaging
作者: Zhang, Shijian1; Zhang, Weifang2; Wang, Yue1; Jin, Zhonghui2; Wang, Xuebin1; Zhang, Junbo1; Zhang, Yanyan2
刊名: BIOCONJUGATE CHEMISTRY
发表日期: 2011-03-01
DOI: 10.1021/bc100357w
卷: 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
所属项目编号: 20771018
项目资助者: National Natural Science Foundation of China ; Fundamental Research Funds for the Central Universities
WOS记录号: WOS:000288401400008
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/56074
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, Key Lab Radiopharmaceut, Minist Educ, Coll Chem, Beijing 100875, Peoples R China
2.Peking Univ, Hosp 3, Dept Nucl Med, Beijing, Peoples R China

Recommended Citation:
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.
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