Tomaž Trobec (Avtor), Kristina Sepčić (Avtor), Monika C. Žužek (Avtor), Jerneja Kladnik (Avtor), Nina Podjed (Avtor), Catarina Cardoso Páscoa (Avtor), Iztok Turel (Avtor), Robert Frangež (Avtor)

Povzetek

Cholinesterases (ChEs) show increased activities in patients with Alzheimer’s disease, and remain one of the main therapeutic targets for treatment of this neurodegenerative disorder. A library of organoruthenium(II) complexes was prepared to investigate the influence of their structural elements on inhibition of ChEs, and on another pharmacologically important group of enzymes, glutathione S-transferases (GSTs). Two groups of organoruthenium(II) compounds were considered: (i) organoruthenium(II) complexes with p-cymene as an arene ligand, and (ii) organoruthenium(II) carbonyl complexes as CO-releasing molecules. Eight organoruthenium complexes were screened for inhibitory activities against ChEs and GSTs of human and animal origins. Some compounds inhibited all of these enzymes at low micromolar concentrations, while others selectively inhibited either ChEs or GSTs. This study demonstrates the importance of the different structural elements of organoruthenium complexes for their inhibitory activities against ChEs and GSTs, and also proposes some interesting compounds for further preclinical testing as ChE or GST inhibitory drugs.

Ključne besede

cholinesterase;enzyme inhibition;glutathione S-transferase;organoruthenium complex;pyrithione;β-diketone;carbonyl;glutathione transferase;

Podatki

Jezik: Angleški jezik
Leto izida:
Tipologija: 1.01 - Izvirni znanstveni članek
Organizacija: UL VF - Veterinarska fakulteta
UDK: 636.09:612
COBISS: 76757507 Povezava se bo odprla v novem oknu
ISSN: 2227-9059
Št. ogledov: 95
Št. prenosov: 38
Ocena: 0 (0 glasov)
Metapodatki: JSON JSON-RDF JSON-LD TURTLE N-TRIPLES XML RDFA MICRODATA DC-XML DC-RDF RDF

Ostali podatki

Sekundarne ključne besede: Cholinesterases;Glutathione Transferase;
Vrsta dela (COBISS): Članek v reviji
Strani: art. 1243, str. 1-18
Letnik: ǂVol. ǂ9
Zvezek: ǂiss. ǂ9
Čas izdaje: 2021
DOI: 10.3390/biomedicines9091243
ID: 15129382