2-Nitroimidazole-tricarbocyanine conjugate as a near-infrared fluorescent probe for in vivo imaging of tumor hypoxia.

Abstract

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.

• Authors: Kensuke Okuda, Yasuyuki Okabe, Tetsuya Kadonosono, Takahiro Ueno, Bahaa G M Youssif, Shinae Kizaka-Kondoh, Hideko Nagasawa
• Journal: Bioconjugate chemistry (Bioconjug Chem) Vol. 23 Issue 3 Pg. 324-9 (Mar 21 2012) ISSN: 1520-4812 [Electronic] United States
• PMID: 22335430 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Carbocyanines
• Fluorescent Dyes
• GPU-167
• Nitroimidazoles

Topics

• Animals
• Carbocyanines (chemistry)
• Cell Hypoxia
• Fluorescent Dyes (chemistry)
• Mice
• Mice, Nude
• Neoplasms (pathology)
• Nitroimidazoles (chemistry)
• Spectroscopy, Near-Infrared (methods)