2-Nitroimidazole-Tricarbocyanine Conjugate as a Near-Infrared Fluorescent Probe for in Vivo Imaging of Tumor Hypoxia

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• 作者：Kensuke Okuda ; Yasuyuki Okabe ; Tetsuya Kadonosono ; Takahiro Ueno ; Bahaa G. M. Youssif ; Shinae Kizaka-Kondoh ; Hideko Nagasawa
• 刊名：Bioconjugate Chemistry
• 出版年：2012
• 出版时间：March 21, 2012
• 年：2012
• 卷：23
• 期：3
• 页码：324-329
• 全文大小：336K
• 年卷期：v.23,no.3(March 21, 2012)
• ISSN：1520-4812

文摘

We developed a novel near-infrared (NIR) fluorescent probe, GPU-167, for in vivo imaging of tumor hypoxia. GPU-167 comprises a tricarbocyanine dye as an NIR fluorophore and two 2-nitroimidazole moieties as exogenous hypoxia markers that undergo bioreductive activation and then selective entrapment in hypoxic cells. After treatment with GPU-167, tumor cells contained significantly higher levels of fluorescence in hypoxia than in normoxia. In vivo fluorescence imaging specifically detected GPU-167 in tumors 24 h after administration. Ex vivo analysis revealed that fluorescence showed a strong correlation with hypoxia inducible factor (HIF)-1 active hypoxic regions. These data suggest that GPU-167 is a promising in vivo optical imaging probe for tumor hypoxia.