1. Academic Validation
  2. NIR-II Emissive Ru(II) Metallacycle Assisting Fluorescence Imaging and Cancer Therapy

NIR-II Emissive Ru(II) Metallacycle Assisting Fluorescence Imaging and Cancer Therapy

  • Small. 2022 Jun;18(23):e2201625. doi: 10.1002/smll.202201625.
Yifan Fan 1 Chonglu Li 1 Suya Bai 2 Xin Ma 1 Jingfang Yang 1 Xiaofang Guan 3 Yao Sun 1


  • 1 Key Laboratory of Pesticides and Chemical Biology (Ministry of Education), College of Chemistryk, Central China Normal University, Wuhan, 430079, China.
  • 2 Key Laboratory of Functional Molecular Solids (Ministry of Education), Anhui Normal University, Wuhu, 241000, China.
  • 3 Zhengzhou Cardiovascular Hospital and 7th People's Hospital of Zhengzhou, Zhengzhou, 450016, China.

Despite the success of emissive Ruthenium (Ru) agents in biomedicine, problems such as the visible-light excitation/emission and single chemo- or phototherapy modality still hamper their applications in deep-tissue imaging and efficient Cancer therapy. Herein, an second nearinfrared window (NIR-II) emissive Ru(II) metallacycle (Ru1000, λem = 1000 nm) via coordination-driven self-assembly is reported, which holds remarkable deep-tissue imaging capability (≈6 mm) and satisfactory chemo-phototherapeutic performance. In vitro results indicate Ru1000 displays promising cellular uptake, good cancer-cell selectivity, attractive anti-metastasis properties, and remarkable anticancer activity against various Cancer cells, including cisplatin-resistant A549 cells (IC50 = 3.4 × 10-6 m vs 92.8 × 10-6 m for cisplatin). The antitumor mechanism could be attributed to Ru1000-induced lysosomal membrane damage and mitochondrial-mediated apoptotic cell death. Furthermore, Ru1000 also allows the high-performance in vivo NIR-II fluorescence imaging-guided chemo-phototherapy against A549 tumors. This work may provide a paradigm for the development of long-wavelength emissive metallacycle-based agents for future biomedicine.


NIR-II; cancer theranostics; metallacycles; self-assembly.