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
Affiliations
  • 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.
PMID: 35560771 DOI: 10.1002/smll.202201625
Abstract

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.

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