New cyclometalated Ru(<scp>ii</scp>) polypyridyl photosensitizers trigger oncosis in cancer cells by inducing damage to cellular membranes

Cervinka, Jakub; Hernández-García, Alba; Bautista, Delia; Markova, Lenka; Kostrhunova, Hana; Malina, Jaroslav; Kasparkova, Jana; Santana, M. Dolores; Brabec, Viktor; Ruiz, José

doi:10.1039/d4qi00732h

Inorg. Chem. Front.

2024

DOI: 10.1039/d4qi00732h

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New cyclometalated Ru(ii) polypyridyl photosensitizers trigger oncosis in cancer cells by inducing damage to cellular membranes

Jakub Cervinka,

Alba Hernández-García,

Delia Bautista

et al.

Abstract: A new generation series of cyclometalated Ru(II) polypyridyl complexes of the type [Ru(C^N)(N^N)2]+, Ru1–Ru4, were rationally designed and synthesized, where N^N = 2,2′-bipyridine (bpy) and dipyrido[3,2-d:2′,3′-f]quinoxaline (dpq) and C^N =...

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Cited by 3 publications

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Ruthenium and platinum-based anticancer metallotherapeutics from the perspectives of photodynamic therapy and bioimaging applications

Ganesan,

Sheela

2024

Chem. Pap.

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Ruthenium and platinum-based anticancer metallotherapeutics from the perspectives of photodynamic therapy and bioimaging applications

Ganesan,

Sheela

2024

Chem. Pap.

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A Novel Substituted Benzo[g]quinoxaline-Based Cyclometalated Ru(II) Complex as a Biocompatible Membrane-Targeted PDT Colon Cancer Stem Cell Agent

Marco,

Kasparkova,

Bautista

et al. 2024

J. Med. Chem.

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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.

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Selenium-containing metallodrug overcomes cervical cancer radioresistance through physical–chemical dual sensitization

Cao,

Guo,

Jiang

et al. 2025

Dalton Trans.

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New cyclometalated Ru(ii) polypyridyl photosensitizers trigger oncosis in cancer cells by inducing damage to cellular membranes

Abstract: A new generation series of cyclometalated Ru(II) polypyridyl complexes of the type [Ru(C^N)(N^N)2]+, Ru1–Ru4, were rationally designed and synthesized, where N^N = 2,2′-bipyridine (bpy) and dipyrido[3,2-d:2′,3′-f]quinoxaline (dpq) and C^N =...

Cited by 3 publications

References 53 publications

Ruthenium and platinum-based anticancer metallotherapeutics from the perspectives of photodynamic therapy and bioimaging applications

Ruthenium and platinum-based anticancer metallotherapeutics from the perspectives of photodynamic therapy and bioimaging applications

A Novel Substituted Benzo[g]quinoxaline-Based Cyclometalated Ru(II) Complex as a Biocompatible Membrane-Targeted PDT Colon Cancer Stem Cell Agent

Selenium-containing metallodrug overcomes cervical cancer radioresistance through physical–chemical dual sensitization

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