High-Throughput Screening of Natural Products Alleviating Acute Liver Injury Using a Polarity-Responsive NIR Ratiometric Fluorescent Probe
Acute liver injury (ALI) is a rapidly progressive inflammatory disease lacking precise noninvasive early diagnostic tools, as traditional enzyme-based tests frequently yield false-positive results. Polarity is a crucial physiological indicator, and its abnormal fluctuations are deeply involved in ALI pathogenesis, necessitating accurate in vivo monitoring. We rationally designed BDP-JL, a new near-infrared ratiometric fluorescent probe featuring a D−π–A architecture for highly sensitive polarity detection. It possesses excellent vesicle-targeting capabilities, enabling precise tracking of polarity dynamics within lipid droplets during ALI progression. With exceptional photostability, low cytotoxicity, and ratiometric signal output that effectively eliminates background interference, BDP-JL achieves accurate real-time imaging of polarity variations in live cells, zebrafish, and mice. Furthermore, we successfully utilized it as an optical platform to screen anti-inflammatory natural products. This work provides a robust noninvasive tool for dynamic polarity monitoring, early ALI diagnosis, and high-throughput drug discovery.
Authors
- Guijin Yao (ORCID: https://orcid.org/0000-0002-2782-5657)
- Jin Zhou (ORCID: https://orcid.org/0000-0001-6761-3408)
- Mingle Li (ORCID: https://orcid.org/0000-0002-0384-9128)
- Hui Li (ORCID: https://orcid.org/0000-0001-9198-3951)
- Juan Chen (ORCID: https://orcid.org/0000-0002-5407-8239)
- Yi Wang (ORCID: https://orcid.org/0000-0002-8023-2586)
- Jianwei Sun (ORCID: https://orcid.org/0000-0002-2470-1077)
- Jianchun Li (ORCID: https://orcid.org/0000-0002-2708-0026)
- Jiale Liu
Institutions
- Shenzhen University (CN)
- Chinese Academy of Medical Sciences & Peking Union Medical College (CN)
- Peking Union Medical College Hospital (CN)
- Second Hospital of Shandong University (CN)
- Weifang People's Hospital (CN)
- Division of Materials Science and Engineering (AU)
- Institute of Medicinal Plant Development (CN)
Publication Details
- Journal
- Journal of Medicinal Chemistry
- Published
- 2026-06-24
- DOI
- https://doi.org/10.1021/acs.jmedchem.6c01343
- Primary Topic
- Molecular Sensors and Ion Detection
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Natural Science Foundation of China
- Natural Science Foundation of Shandong Province
- Wuhan National Laboratory for Optoelectronics
- Taishan Scholar Project of Shandong Province