Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry , Beijing Normal University , Beijing 100875 , People's Republic of China.
College of Science , Liaoning Technical University , Fuxin 123000 , People's Republic of China.
Inorg Chem. 2019 Oct 21;58(20):14244-14259. doi: 10.1021/acs.inorgchem.9b02420. Epub 2019 Oct 9.
Near-IR-emitting and/or efficiently photodynamic water-soluble Ru(II) complexes that hold great application potentials as photodynamic therapy and/or photodetection agents for cancers have been poorly explored. In this paper, the solvatochromism, calf thymus DNA binding, and singlet oxygen generation properties of a known ruthenium(II) complex of visible-emitting Ru(bpy)(dtdpq) () and a new homoleptic complex of near-IR-emitting Ru(dtdpq) () (bpy = 2,2'-bipyridine, dtdpq = 2,3-bis(thiophen-2-yl)pyrazino[2,3-][1,10]phenanothroline) in water are reported. Moreover, DNA photocleavage, singlet oxygen generation in HeLa cells, cellular uptake/localization, and in vitro photodynamic therapy for cancer cells of water-soluble are described in detail. The results show that acted as potent photodynamic cancer therapy and mitochondrial imaging agents. exhibited very strong solvatochromism from a visible emission maximum at 588 nm in CHCl to the near-IR region at 700 nm in water and singlet oxygen generation yield in water (23%) and DNA binding properties (intercalative DNA binding constant on the order of 10 M) comparable to those of , which should make attractive for the aforementioned applications of if the water solubility of can be improved enough for the studies above.
近红外发光和/或高效光动力水溶性钌（II）配合物作为光动力治疗和/或癌症光检测试剂具有巨大的应用潜力，但尚未得到充分探索。本文报道了一种已知的可见发光Ru(bpy)(dtdpq)()（bpy=2,2'-联吡啶，dtdpq=2,3-双（噻吩-2-基）吡嗪[2,3-][1,10]菲咯啉）的钌（II）配合物和一种新的近红外发光同核配合物Ru(dtdpq)()（ ）在水中的溶剂化变色、小牛胸腺 DNA 结合和单线态氧生成性质。此外，详细描述了水溶性 在 HeLa 细胞中的 DNA 光解、单线态氧生成、细胞摄取/定位以及体外光动力治疗癌症。结果表明， 充当有效的光动力癌症治疗和线粒体成像剂。 在水中从 588nm 的可见发射最大值到 700nm 的近红外区域显示出很强的溶剂化变色，并且在水中具有较高的单线态氧生成效率（23%）和 DNA 结合性质（与 相当的插入型 DNA 结合常数约为 10 M），如果 能够提高足够的水溶性，使其能够满足上述研究的要求，那么 应该会在上述应用中很有吸引力。
