School of Basic Medical Sciences, Guangdong Pharmaceutical University, Guangzhou, Guangdong 510006, P.R China.
School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, Shenzhen, Guangdong 518107, P.R China.
J Med Chem. 2024 Aug 8;67(15):13435-13445. doi: 10.1021/acs.jmedchem.4c01307. Epub 2024 Jul 30.
Photodynamic therapy has been regarded as a noninvasive treatment for cancer with spatiotemporal control over drug activation. Bis-terpyridyl Ru(II) complexes exhibit a promising achiral structure but suffer from low photoreactivity due to deviation from the ideal octahedral geometry. Herein, we introduce the donor-acceptor-donor motif to construct a dinuclear bis-terpyridyl Ru(II) complex (). exhibits superior light absorption properties compared with mononuclear complex . Importantly, upon 595 nm light excitation, shows promising synergetic type I/II photosensitization and photocatalytic activity, while is inactive. Anticancer mechanistic studies reflect that induces intracellular redox imbalance and affects the biosynthetic and metabolic processes, leading to cell apoptosis. Overall, this work provides a simple strategy to rouse the PDT efficiency of bis-terpyridyl Ru(II) complexes.
光动力疗法被认为是一种具有时空控制药物激活能力的非侵入性癌症治疗方法。双-二吡啶钌(II)配合物具有很有前途的手性结构，但由于偏离理想的八面体几何形状，其光反应性较低。在此，我们引入给体-受体-给体结构来构建双核双-二吡啶钌(II)配合物()。与单核配合物相比，表现出优异的光吸收性能。重要的是，在 595nm 光激发下，表现出有前景的协同 I/II 型光动力和光催化活性，而则没有活性。抗癌机制研究反映出诱导细胞内氧化还原失衡并影响生物合成和代谢过程，导致细胞凋亡。总的来说，这项工作提供了一种简单的策略来提高双-二吡啶钌(II)配合物的光动力疗法效率。
