J 2020

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

MASURI, Sebastiano, Enzo CADONI, Maria Grazia CABIDDU, Francesco ISAIA, Maria Giovanna DEMURU et. al.

Basic information

Original name

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

Authors

MASURI, Sebastiano (380 Italy), Enzo CADONI (380 Italy), Maria Grazia CABIDDU (380 Italy), Francesco ISAIA (380 Italy), Maria Giovanna DEMURU (380 Italy), Lukáš MORÁŇ (203 Czech Republic, belonging to the institution), David BUČEK (203 Czech Republic), Petr VAŇHARA (203 Czech Republic, belonging to the institution), Josef HAVEL (203 Czech Republic, belonging to the institution) and Tiziana PIVETTA (380 Italy, guarantor)

Edition

Metallomics, Cambridge, Royal Society of Chemistry, 2020, 1756-5901

Other information

Language

English

Type of outcome

Článek v odborném periodiku

Field of Study

10600 1.6 Biological sciences

Country of publisher

United States of America

Confidentiality degree

není předmětem státního či obchodního tajemství

References:

Impact factor

Impact factor: 4.526

RIV identification code

RIV/00216224:14110/20:00116696

Organization unit

Faculty of Medicine

UT WoS

000542894500004

Keywords in English

Unfolded Protein Response; X Box Binding Protein 1; Activating Transcription Factor 6

Tags

International impact, Reviewed
Změněno: 27/1/2021 10:09, Mgr. Tereza Miškechová

Abstract

V originále

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.

Links

LM2018129, research and development project
Name: Národní infrastruktura pro biologické a medicínské zobrazování Czech-BioImaging
Investor: Ministry of Education, Youth and Sports of the CR