64Cu-Labeled triphenylphosphonium and triphenylarsonium cations as highly tumor-selective imaging agents.
64Cu-Labeled triphenylphosphonium and triphenylarsonium cations as highly tumor-selective imaging agents.
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DOI：
10.1021/jm0704088
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发表时间：
2007-09
影响因子：
7.3
通讯作者：
Jianjun Wang;Chang-Tong Yang;Young-Seung Kim;S. G. Sreerama;Qizhen Cao;Zibo Li;Zhengjie He;Xiaoyuan C
中科院分区：
文献类型：
--
作者：
Jianjun Wang;Chang-Tong Yang;Young-Seung Kim;S. G. Sreerama;Qizhen Cao;Zibo Li;Zhengjie He;Xiaoyuan C
This report presents synthesis and evaluation of the 64Cu-labeled triphenylphosphonium (TPP) cations as new radiotracers for imaging tumors by positron emission tomography. Biodistribution properties of 64Cu-L1, 64Cu-L2, 64Cu-L3, and 99mTc-Sestamibi were evaluated in athymic nude mice bearing U87MG human glioma xenografts. The most striking difference is that 64Cu-L1, 64Cu-L2, and 64Cu-L3 have much lower heart uptake (30 min p.i. Their tumor/heart ratios increase steadily from approximately 1 at 5 min p.i. to approximately 5 at 120 min p.i. The tumor/heart ratio of 64Cu-L3 is approximately 40 times better than that of 99mTc-Sestamibi at 120 min postinjection. Results from in vitro assays show that 64Cu-L1 is able to localize in tumor mitochondria. The tumor is clearly visualized in the tumor-bearing mice administered with 64Cu-L1 as 30 min postinjection. The 64Cu-labeled TPP/TPA cations are very selective radiotracers that are able to provide the information of mitochondrial bioenergetic function in tumors by monitoring mitochondrial potential in a noninvasive fashion.
