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Fine tuning of cholinesterase and glutathione-S-transferase activities by organoruthenium(II) complexes

2021-09-16Artigo científico Acesso aberto
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dc.contributor.authorTrobec, Tomaž
dc.contributor.authorSepčić, Kristina
dc.contributor.authorŽužek, Monika Cecilija
dc.contributor.authorKladnik, Jerneja
dc.contributor.authorPodjed, Nina
dc.contributor.authorPáscoa, Catarina Cardoso
dc.contributor.authorTurel, Iztok
dc.contributor.authorFrangež, Robert
dc.contributor.institutionDQ - Departamento de Química
dc.contributor.pblMDPI AG
dc.date.accessioned2022-08-01T22:26:00Z
dc.date.available2022-08-01T22:26:00Z
dc.date.issued2021-09-16
dc.descriptionP4-0053 P1-0207 P1-0175 51852 39077
dc.description.abstractCholinesterases (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 li-brary 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 consid-ered: (i) organoruthenium(II) complexes with p-cymene as an arene ligand, and (ii) organoruthe-nium(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.en
dc.description.versionpublishersversion
dc.description.versionpublished
dc.format.extent769873
dc.identifier.doi10.3390/biomedicines9091243
dc.identifier.issn2227-9059
dc.identifier.otherPURE: 45749929
dc.identifier.otherPURE UUID: 8f32a431-2f34-495b-a06c-d9d62fef333e
dc.identifier.otherScopus: 85115240287
dc.identifier.otherPubMed: 34572429
dc.identifier.otherPubMedCentral: PMC8467340
dc.identifier.otherWOS: 000700573100001
dc.identifier.urihttp://hdl.handle.net/10362/142771
dc.identifier.urlhttps://www.scopus.com/pages/publications/85115240287
dc.language.isoeng
dc.peerreviewedyes
dc.subjectCarbonyl
dc.subjectCholinesterase
dc.subjectEnzyme inhibition
dc.subjectGlutathione S-transferase
dc.subjectOrganoruthenium complex
dc.subjectPyrithione
dc.subjectβ-diketone
dc.subjectMedicine (miscellaneous)
dc.subjectGeneral Biochemistry,Genetics and Molecular Biology
dc.subjectSDG 3 - Good Health and Well-being
dc.titleFine tuning of cholinesterase and glutathione-S-transferase activities by organoruthenium(II) complexesen
dc.typejournal article
degois.publication.issue9
degois.publication.titleBiomedicines
degois.publication.volume9
dspace.entity.typePublication
rcaap.rightsopenAccess

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