Most cited article - PubMed ID 35502218
Gallium(III) Complex with Cloxyquin Ligands Induces Ferroptosis in Cancer Cells and Is a Potent Agent against Both Differentiated and Tumorigenic Cancer Stem Rhabdomyosarcoma Cells
Herein, we describe and investigate biological activity of three octahedral ruthenium(II) complexes of the type [Ru(C∧N)(phen)2]+, RuL1-RuL3, containing a π-expansive cyclometalating substituted benzo[g]quinoxaline ligand (C∧N ligand) (phen = 1,10-phenanthroline). Compounds RuL1-RuL3 in cervical, melanoma, and colon human cancer cells exhibit high phototoxicity after irradiation with light (particularly blue), with the phototoxicity index reaching 100 for the complex RuL2 in most sensitive HCT116 cells. RuL2 accumulates in the cellular membranes. If irradiated, it induces lipid peroxidation, likely connected with photoinduced ROS generation. Oxidative damage to the fatty acids leads to the attenuation of the membranes, the activation of caspase 3, and the triggering of the apoptotic pathway, thus implementing membrane-localized photodynamic therapy. RuL2 is the first photoactive ruthenium-based complex capable of killing the hardly treatable colon cancer stem cells, a highly resilient subpopulation within a heterogeneous tumor mass, responsible for tumor recurrence and the metastatic progression of cancer.
- MeSH
- Apoptosis drug effects MeSH
- Cell Membrane drug effects metabolism MeSH
- Quinoxalines * chemistry pharmacology chemical synthesis MeSH
- Photochemotherapy * MeSH
- Photosensitizing Agents * pharmacology chemistry chemical synthesis therapeutic use MeSH
- Coordination Complexes * pharmacology chemistry chemical synthesis therapeutic use MeSH
- Humans MeSH
- Cell Line, Tumor MeSH
- Neoplastic Stem Cells * drug effects pathology MeSH
- Colonic Neoplasms * drug therapy pathology MeSH
- Antineoplastic Agents * pharmacology chemistry chemical synthesis therapeutic use MeSH
- Reactive Oxygen Species metabolism MeSH
- Ruthenium * chemistry pharmacology MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Quinoxalines * MeSH
- Photosensitizing Agents * MeSH
- Coordination Complexes * MeSH
- Antineoplastic Agents * MeSH
- Reactive Oxygen Species MeSH
- Ruthenium * MeSH
