Drug-induced
liver injury (DILI) is a widespread clinical problem.
The pathophysiological mechanisms of DILI are complicated, and the
traditional diagnostic methods for DILI have their limitations. Owing
to its convenient operation, high sensitivity, and high specificity,
luminescent sensing and imaging as an indispensable tool in biological
research and clinical trials may provide an important means for DILI
study. Herein, we report the rational design and preparation of a
near-infrared dual-phosphorescent polymeric probe (P-ONOO) for exploring the DILI via specific imaging of peroxynitrite (ONOO–) elevation in vivo, which was one of early markers
of DILI and very difficult to be detected due to its short half-life
and high reactive activity. With the utilization of P-ONOO, the raised ONOO– was visualized successfully
in the drug-treated hepatocytes with a high signal-to-noise ratio
via ratiometric and time-resolved photoluminescence imaging. Importantly,
the ONOO– boost in the acetaminophen-induced liver
injury in real time was verified, and the direct observation of the
elevated ONOO– production in ketoconazole-induced
liver injury was achieved for the first time. Our findings may contribute
to understanding the exact mechanism of ketoconazole-induced hepatotoxicity
that is still ambiguous. Notably, this luminescent approach for revealing
the liver injury works fast and conveniently.