The first copper(II) complex with 1,10-phenanthroline and salubrinal with interesting biochemical properties.

Warning

This publication doesn't include Faculty of Sports Studies. It includes Faculty of Medicine. Official publication website can be found on muni.cz.
Authors

MASURI Sebastiano CADONI Enzo CABIDDU Maria Grazia ISAIA Francesco DEMURU Maria Giovanna MORÁŇ Lukáš BUČEK David VAŇHARA Petr HAVEL Josef PIVETTA Tiziana

Year of publication 2020
Type Article in Periodical
Magazine / Source Metallomics
MU Faculty or unit

Faculty of Medicine

Citation
Web https://doi.org/10.1039/D0MT00006J
Doi http://dx.doi.org/10.1039/d0mt00006j
Keywords Unfolded Protein Response; X Box Binding Protein 1; Activating Transcription Factor 6
Description The novel copper complex [Cu(phen)(2)(salubrinal)](ClO4)(2)(C0SAL) has been synthesised and characterised. Copper(ii) is coordinated by salubrinal through the thionic group, as shown by the UV-Vis, IR, ESI-MS and tandem mass results, together with the theoretical calculations. The formed complex showed a DPPH radical scavenging ability higher than that of salubrinal alone. Studies on lipid oxidation inhibition showed that theC0SALconcentration, required to inhibit the enzyme, was lower than that of salubrinal. The inhibition of the enzyme could take placeviaallosteric modulation, as suggested by docking calculations.C0SALshowed a good cytotoxic activity on A2780 cells, 82 fold higher than that of the precursor salubrinal and 1.4 fold higher than that of [Cu(phen)(2)(H2O)](ClO4)(2). Treatment withC0SALin SKOV3 ovarian cancer cells induced expression of GRP-78 and DDIT3 regulators of ER-stress response. The cytotoxic effect ofC0SALwas reverted in the presence of TUDCA, suggesting thatC0SALinduces cell death through ER-stress. In A2780 cells treated withC0SAL gamma-H2AX was accumulated, suggesting that DNA damage was also involved.
Related projects:

You are running an old browser version. We recommend updating your browser to its latest version.

More info