4.7 Article

A dual-channel fluorescent ratio probe with hypoxia targeting and hypoxia activation capacity for tumour imaging

Journal

POLYMER CHEMISTRY
Volume 13, Issue 22, Pages 3358-3366

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/d2py00313a

Keywords

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Funding

  1. National Natural Science Foundation of China [51973188, 21774109]
  2. Zhejiang University Education Foundation Global Partnership Fund
  3. China Postdoctoral Science Foundation [2019M662088]
  4. Natural Science Foundation of Zhejiang Province [LR18E030002]

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This study for the first time employed a dual-channel NIR probe for effective prolonged hypoxia ratio imaging. The probe had hypoxia targeting and activation capacity, allowing monitoring of probe distribution and activation in the hypoxic tumor microenvironment.
Efficient hypoxia diagnosis is a great challenge for nearly all solid tumours due to operability, permeability and specificity. Although some inspiring approaches have been explored to date, it is the first time that a dual-channel NIR probe (denoted as OPDEA/BOD-NO2) simultaneously with hypoxia targeting and activation capacity was employed to realize effective prolonged hypoxia ratio imaging in the present work. OPDEA/BOD-NO2 consists of hypoxia-targeting tertiary amine N-oxide based polymers and nitrobenzene modified Aza-BODIPY (BOD-NO2). OPDEA/BOD-NO2 had strong red fluorescence at lambda(ex) = 660 nm and lambda(em) = 710 nm, while it turned into another fluorescent Aza-BODIPY dye (BOD) with strong NIR fluorescence at Rex = 720 nm and A em = 790 nm in hypoxia microenvironment, providing two channels with big Stokes shift for hypoxia ratio imaging and monitoring probe distribution and activation, respectively. Meanwhile, hypoxia-targeting tertiary amine N-oxide based polymers could effectively enhance tumour accumulation (2.99-fold, 660 nm; and 2.74-fold, 720 nm) for prolonged hypoxia ratio imaging with obviously improved signal-to-background ratio within 48 hours, which is much better than that of PEG/BOD-NO2.

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