J 2023

A novel heteroleptic Cu(II)-phenanthroline-UDCA complex as lipoxygenase inhibitor and ER-stress inducer in cancer cell lines

MASURI, Sebastiano, Lukáš MORÁŇ, Tereza VESSELÁ, Enzo CADONI, Maria Grazia CABIDDU et. al.

Basic information

Original name

A novel heteroleptic Cu(II)-phenanthroline-UDCA complex as lipoxygenase inhibitor and ER-stress inducer in cancer cell lines

Authors

MASURI, Sebastiano, Lukáš MORÁŇ (203 Czech Republic, belonging to the institution), Tereza VESSELÁ (203 Czech Republic, belonging to the institution), Enzo CADONI, Maria Grazia CABIDDU, Lukáš PEČINKA (203 Czech Republic, belonging to the institution), Viktorie GABRIELOVÁ (203 Czech Republic, belonging to the institution), Francesca MELONI, Josef HAVEL (203 Czech Republic, belonging to the institution), Petr VAŇHARA (203 Czech Republic, belonging to the institution) and Tiziana PIVETTA (guarantor)

Edition

Journal of Inorganic Biochemistry, New York, Elsevier, 2023, 0162-0134

Other information

Language

English

Type of outcome

Článek v odborném periodiku

Field of Study

10601 Cell biology

Country of publisher

United States of America

Confidentiality degree

není předmětem státního či obchodního tajemství

References:

Impact factor

Impact factor: 3.900 in 2022

RIV identification code

RIV/00216224:14110/23:00131184

Organization unit

Faculty of Medicine

UT WoS

001032239600001

Keywords in English

Copper complex; Solution equilibria; Mass spectrometry; Lipoxygenase; Molecular docking; ER stress

Tags

Tags

International impact, Reviewed
Změněno: 1/2/2024 12:20, Mgr. Tereza Miškechová

Abstract

V originále

A new heteroleptic copper(II) compound named C0-UDCA was prepared by reaction of [Cu(phen)2(OH2)](ClO4)2 (C0) with the bile ursodeoxycholic acid (UDCA). The resulting compound is able to inhibit the lipoxygenase enzyme showing more efficacy than the precursors C0 and UDCA. Molecular docking simulations clarified the interactions with the enzyme as due to allosteric modulation. The new complex shows antitumoral effect on ovarian (SKOV-3) and pancreatic (PANC-1) cancer cells at the Endoplasmic Reticulum (ER) level by activating the Unfolded Protein Response. In particular, the chaperone BiP, the pro-apoptotic protein CHOP and the transcription factor ATF6 are upregulated in the presence of C0-UDCA. The combination of Intact Cell MALDI-MS and statistical analysis have allowed us to discriminate between untreated and treated cells based on their mass spectrometry fingerprints.

Links

MUNI/A/1298/2022, interní kód MU
Name: Základní a aplikovaný výzkum a vývoj metod chemické a fyzikálně chemické analýzy pro studium přírody a pokročilé technologie
Investor: Masaryk University, Basic and applied research and development of chemical and physicochemical analytical methods for the study of nature and advanced technology
MUNI/A/1301/2022, interní kód MU
Name: Zdroje pro tkáňové inženýrství 13
Investor: Masaryk University
MUNI/11/ACC/3/2022, interní kód MU
Name: Bioanalytical quality control of cGMP/ATMP-grade stem cells and progenitors
Investor: Masaryk University, Accelerate
NU23-08-00241, research and development project
Name: Vývoj ex-vivo buněčných modelů pro adenokarcinom pankreatu: markery a cíle pro precizní medicínu
Investor: Ministry of Health of the CR, Development of ex vivo cellular models for pancreatic adenocarcinoma: markers and targets for precision medicine, Subprogram 1 - standard
ROZV/28/LF/2020, interní kód MU
Name: LF - Příspěvek na InstP 2020
Investor: Ministry of Education, Youth and Sports of the CR, Internal development projects