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Copper(I) complexes with phosphine derived from sparfloxacin. Part III: multifaceted cell death and preliminary study of liposomal formulation of selected copper(I) complex

Abstract

Cytotoxic effect of iodide or thiocyanate copper(I) complexes (1-PSf, 2-PSf, 3-PSf, 4-PSf) with a phosphine derived from sparfloxacin (HSf) and 2,9-dimethyl-1,10-phenanthroline (dmp) or 2,2’-biquinoline (bq) as diimine auxiliary ligands was proved in vitro on somatic (MRC-5) and neoplastic (MCF7) human cell lines. Differences in mode of action were investigated in-depth for selected the dmp and the bq complexes (1-PSf, 3-PSf, respectively) by elucidation of (i) efficiency to produce reactive oxygen species (ROS) in biological systems (cyclic voltammetry), (ii) their impact on mitochondrial membrane potential, (iii) potency to activation of caspases 3 and 9, and (iv) influence on the degree of DNA degradation (comet assay). It was concluded that the apoptosis of cancer cells is straightly connected with caspase-dependent mitochondrial pathway and supported by ROS production along with irreversible DNA fragmentations. Finally, it was demonstrated that the selected copper(I) complex encapsulated inside liposomes (1-PSf-L) exhibited the enhanced accumulation inside cancer cells. This resulted in its higher cytotoxicity against cancer cells with therapeutic index even ca. 60. Increased selective accumulation in active neoplasm with simultaneous enhanced bioavailability and reduced systemic toxicity of liposomal formulations of copper(I) complexes can result in development of new copper-based therapeutics and their successful implementation in anticancer chemotherapy.

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Supplementary files

Publication details

The article was received on 18 Oct 2017, accepted on 21 Dec 2017 and first published on 26 Dec 2017


Article type: Paper
DOI: 10.1039/C7DT03917D
Citation: Dalton Trans., 2017, Accepted Manuscript
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    Copper(I) complexes with phosphine derived from sparfloxacin. Part III: multifaceted cell death and preliminary study of liposomal formulation of selected copper(I) complex

    A. Kyzioł, A. Cierniak, J. Gubernator, A. Markowski, M. Jezowska-Bojczuk and U. K. Komarnicka, Dalton Trans., 2017, Accepted Manuscript , DOI: 10.1039/C7DT03917D

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