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Near-IR/Visible-Emitting Thiophenyl-Based Ru(II) Complexes: Efficient Photodynamic Therapy, Cellular Uptake, and DNA
Si-Qi Zhang1, Ting-Ting Meng1,2, Jia Li3
1Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry , Beijing Normal University , Beijing 100875 , People's Republic of China.
Inorganic Chemistry
|October 10, 2019
Summary
This study explores water-soluble ruthenium(II) complexes for cancer photodynamic therapy. Ru1 shows potent cancer therapy and imaging capabilities, while Ru2 exhibits promising near-IR emission and singlet oxygen generation for potential therapeutic applications.
Area of Science:
- Coordination Chemistry
- Photochemistry
- Biomedical Applications
Background:
- Near-infrared (NIR) emitting and photodynamically active water-soluble ruthenium(II) complexes are underexplored for cancer photodynamic therapy (PDT) and photodetection.
- Ruthenium(II) complexes offer potential due to their tunable photophysical properties and biological compatibility.
Purpose of the Study:
- To investigate the photophysical properties, DNA binding, and singlet oxygen generation of visible-emitting [Ru(bpy)2(dtdpq)](ClO4)2 (Ru1) and near-IR-emitting [Ru(dtdpq)3](ClO4)2 (Ru2) complexes in water.
- To evaluate the in vitro photodynamic therapy efficacy, cellular uptake, and localization of Ru1 in cancer cells.
- To assess the potential of Ru2 as a NIR-emitting agent for PDT and photodetection.
Main Methods:
- Synthesis and characterization of ruthenium(II) complexes.
- Solvatochromism studies, calf thymus DNA binding assays, and singlet oxygen generation yield measurements.
- DNA photocleavage assays, cellular uptake and localization studies in HeLa cells, and in vitro photodynamic therapy experiments.
Main Results:
- Ru1 demonstrated potent photodynamic cancer therapy and mitochondrial imaging capabilities.
- Ru2 exhibited significant solvatochromism, shifting emission from visible to NIR (700 nm in water).
- Ru2 showed a singlet oxygen generation yield of 23% in water and intercalative DNA binding (10^6 M^-1), comparable to Ru1.
Conclusions:
- Ru1 is a promising agent for photodynamic cancer therapy and mitochondrial imaging.
- Ru2's NIR emission and photodynamic properties make it attractive for PDT and photodetection, pending improved water solubility.
- Further development of water-soluble Ru(II) complexes is crucial for advancing their clinical applications in cancer treatment.
