The first copper(II) complex with 1,10-phenanthroline and salubrinal with interesting biochemical properties.
| Autoři | |
|---|---|
| Rok publikování | 2020 |
| Druh | Článek v odborném periodiku |
| Časopis / Zdroj | Metallomics |
| Fakulta / Pracoviště MU | |
| Citace | |
| www | https://doi.org/10.1039/D0MT00006J |
| Doi | http://dx.doi.org/10.1039/d0mt00006j |
| Klíčová slova | Unfolded Protein Response; X Box Binding Protein 1; Activating Transcription Factor 6 |
| Popis | 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. |
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