In vitro and in vivo evaluation of a Cu-64-labeled propylene amine oxime complex as a potential hypoxia imaging agent bearing two 3-nitrotriazole groups

In vitro and in vivo evaluation of a Cu-64-labeled propylene amine oxime complex as a potential hypoxia imaging agent bearing two 3-nitrotriazole groups
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Cu-64 标记的丙胺肟复合物作为带有两个 3-硝基三唑基团的潜在缺氧显像剂的体外和体内评估

DOI:
10.1007/s10967-017-5345-4
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发表时间:
2017
影响因子:
1.6
通讯作者:
Chu Taiwei
Chu Taiwei
中科院分区:
化学4区
文献类型:
--
作者:
Zhang Wei;Zhang Qiang;Chen Qingxin;Zhu Hua;Yang Zhi;Chu Taiwei

文献摘要

被引文献

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用64 CuCl 2标记了丙烯胺肟(PnAO)配体PnAO-1,1′-双(3-硝基三唑)(3 P3)。体外实验结果表明,64 Cu-3 P3可在缺氧的S180肿瘤细胞中蓄积。~(64)Cu-3P_3在荷S180肿瘤小鼠体内的生物分布研究表明,肿瘤摄取、肿瘤-肌肉比和肿瘤-血液比是相当大的。在给药后18小时的正电子发射断层扫描成像中也可以发现肿瘤区域。作为对比,还研究了经典的乏氧显像剂64 Cu-ATSM。实验结果表明,~(64)Cu-3P_3有可能成为一种有效的乏氧显像剂。
The propylene amine oxime (PnAO) ligand, PnAO-1, 1′-bis(3-nitrotriazole) (3P3) with two 3-nitrotriazole groups was labeled with64CuCl2. In vitro results suggest that64Cu-3P3 can accumulate in hypoxic S180 tumor cells. Biodistribution studies of64Cu-3P3 in mice bearing S180 tumor demonstrate that the tumor uptake, tumor-to-muscle ratio, and tumor-to-blood ratio are considerable. A tumor area could also be found in positron emission tomography imaging 18 h post-administration. For comparison, the classical hypoxia imaging agent64Cu-ATSM was also investigated. The experimental data obtained demonstrate that64Cu-3P3 may potentially be used as an efficient hypoxia imaging agent.