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

Abstract

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.

Keywords

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

Data

Language: English
Year of publishing:
Typology: 1.01 - Original Scientific Article
Organization: UL VF - Veterinary Faculty
UDC: 636.09:612
COBISS: 76757507 Link will open in a new window
ISSN: 2227-9059
Views: 95
Downloads: 38
Average score: 0 (0 votes)
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Other data

Secondary keywords: Cholinesterases;Glutathione Transferase;
Type (COBISS): Article
Pages: art. 1243, str. 1-18
Volume: ǂVol. ǂ9
Issue: ǂiss. ǂ9
Chronology: 2021
DOI: 10.3390/biomedicines9091243
ID: 15129382