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@article{1686140,
author = {Masuri, Sebastiano and Cadoni, Enzo and Cabiddu, Maria Grazia and Isaia, Francesco and Demuru, Maria Giovanna and Moráň, Lukáš and Buček, David and Vaňhara, Petr and Havel, Josef and Pivetta, Tiziana},
article_location = {Cambridge},
article_number = {6},
doi = {http://dx.doi.org/10.1039/d0mt00006j},
keywords = {Unfolded Protein Response; X Box Binding Protein 1; Activating Transcription Factor 6},
language = {eng},
issn = {1756-5901},
journal = {Metallomics},
title = {The first copper(II) complex with 1,10-phenanthroline and salubrinal with interesting biochemical properties.},
url = {https://doi.org/10.1039/D0MT00006J},
volume = {12},
year = {2020}
}
TY - JOUR
ID - 1686140
AU - Masuri, Sebastiano - Cadoni, Enzo - Cabiddu, Maria Grazia - Isaia, Francesco - Demuru, Maria Giovanna - Moráň, Lukáš - Buček, David - Vaňhara, Petr - Havel, Josef - Pivetta, Tiziana
PY - 2020
TI - The first copper(II) complex with 1,10-phenanthroline and salubrinal with interesting biochemical properties.
JF - Metallomics
VL - 12
IS - 6
SP - 891-901
EP - 891-901
PB - Royal Society of Chemistry
SN - 17565901
KW - Unfolded Protein Response
KW - X Box Binding Protein 1
KW - Activating Transcription Factor 6
UR - https://doi.org/10.1039/D0MT00006J
L2 - https://doi.org/10.1039/D0MT00006J
N2 - 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.
ER -
MASURI, Sebastiano, Enzo CADONI, Maria Grazia CABIDDU, Francesco ISAIA, Maria Giovanna DEMURU, Lukáš MORÁŇ, David BUČEK, Petr VAŇHARA, Josef HAVEL and Tiziana PIVETTA. The first copper(II) complex with 1,10-phenanthroline and salubrinal with interesting biochemical properties. \textit{Metallomics}. Cambridge: Royal Society of Chemistry, 2020, vol.~12, No~6, p.~891-901. ISSN~1756-5901. Available from: https://dx.doi.org/10.1039/d0mt00006j.
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