Development of a Hypoxia-Selective Near-Infrared Fluorescent Probe for Non-invasive Tumor Imaging

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概要

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• A near-infrared fluorochrome, GPU-311, was designed, synthesized and evaluated for its application in non-invasive imaging of tumor hypoxia. Efficient synthesis was achieved by nucleophilic substitution and click chemistry ring using the bifunctional tetraethylene glycol linker 2 containing thiol and azide groups for the conjugation of the propargylated nitroimidazole 1 and the heptamethine cyanine dye 3 bearing a 2-chloro-1-cyclohexenyl ring. GPU-311 exhibited long excitation and emission wavelength (Ex/Em=785/802 nm) and a decent quantum yield (0.05). The water solubility and hydrophilicity of GPU-311 increased. After in vitro treatment of SUIT-2/HRE-Luc pancreatic cancer cells with GPU-311, a higher level of fluorescence was observed selectively in hypoxia than in normoxia. However, in vivo fluorescence imaging of a mouse xenograft model after GPU-311 administration revealed inadequate accumulation of GPU-311 in tumors due to its rapid elimination through the liver.

著者

• Nagasawa Hideko

  Laboratory Of Medicinal And Pharmaceutical Chemistry Gifu Pharmaceutical University

• Hussein Mostafa

  Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University

• Salem Ola

  Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University

• Hayallah Alaa

  Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University

• Youssif Bahaa

  Laboratory of Medicinal and Pharmaceutical Chemistry, Gifu Pharmaceutical University

• Okuda Kensuke

  Laboratory of Medicinal and Pharmaceutical Chemistry, Gifu Pharmaceutical University

• Kadonosono Tetsuya

  Division of Biofunctional Engineering, School of Bioscience and Biotechnology, Tokyo Institute of Technology

• Kizaka-Kondoh Shinae

  Division of Biofunctional Engineering, School of Bioscience and Biotechnology, Tokyo Institute of Technology

• Nagasawa Hideko

  Laboratory of Medicinal and Pharmaceutical Chemistry, Gifu Pharmaceutical University

関連論文

• Design of Hypoxia-Targeting Drugs as New Cancer Chemotherapeutics
• Pathophysiological Response to Hypoxia-From the Molecular Mechanisms of Malady to Drug Discovery : Drug Discovery for Targeting the Tumor Microenvironment
• Development of a Hypoxia-Selective Near-Infrared Fluorescent Probe for Non-invasive Tumor Imaging
• Isolation of Six Isoprenylated Biflavonoids from the Leaves of Garcinia subelliptica

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