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

Detalhes bibliográficos
Autor(a) principal: Trobec, Tomaž
Data de Publicação: 2021
Outros Autores: Sepčić, Kristina, Žužek, Monika Cecilija, Kladnik, Jerneja, Podjed, Nina, Páscoa, Catarina Cardoso, Turel, Iztok, Frangež, Robert
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10362/142771
Resumo: P4-0053 P1-0207 P1-0175 51852 39077
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spelling Fine tuning of cholinesterase and glutathione-S-transferase activities by organoruthenium(II) complexesCarbonylCholinesteraseEnzyme inhibitionGlutathione S-transferaseOrganoruthenium complexPyrithioneβ-diketoneMedicine (miscellaneous)Biochemistry, Genetics and Molecular Biology(all)SDG 3 - Good Health and Well-beingP4-0053 P1-0207 P1-0175 51852 39077Cholinesterases (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.DQ - Departamento de QuímicaRUNTrobec, TomažSepčić, KristinaŽužek, Monika CecilijaKladnik, JernejaPodjed, NinaPáscoa, Catarina CardosoTurel, IztokFrangež, Robert2022-08-01T22:26:00Z2021-09-162021-09-16T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10362/142771eng2227-9059PURE: 45749929https://doi.org/10.3390/biomedicines9091243info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2024-03-11T05:20:40Zoai:run.unl.pt:10362/142771Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T03:50:30.678903Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv Fine tuning of cholinesterase and glutathione-S-transferase activities by organoruthenium(II) complexes
title Fine tuning of cholinesterase and glutathione-S-transferase activities by organoruthenium(II) complexes
spellingShingle Fine tuning of cholinesterase and glutathione-S-transferase activities by organoruthenium(II) complexes
Trobec, Tomaž
Carbonyl
Cholinesterase
Enzyme inhibition
Glutathione S-transferase
Organoruthenium complex
Pyrithione
β-diketone
Medicine (miscellaneous)
Biochemistry, Genetics and Molecular Biology(all)
SDG 3 - Good Health and Well-being
title_short Fine tuning of cholinesterase and glutathione-S-transferase activities by organoruthenium(II) complexes
title_full Fine tuning of cholinesterase and glutathione-S-transferase activities by organoruthenium(II) complexes
title_fullStr Fine tuning of cholinesterase and glutathione-S-transferase activities by organoruthenium(II) complexes
title_full_unstemmed Fine tuning of cholinesterase and glutathione-S-transferase activities by organoruthenium(II) complexes
title_sort Fine tuning of cholinesterase and glutathione-S-transferase activities by organoruthenium(II) complexes
author Trobec, Tomaž
author_facet Trobec, Tomaž
Sepčić, Kristina
Žužek, Monika Cecilija
Kladnik, Jerneja
Podjed, Nina
Páscoa, Catarina Cardoso
Turel, Iztok
Frangež, Robert
author_role author
author2 Sepčić, Kristina
Žužek, Monika Cecilija
Kladnik, Jerneja
Podjed, Nina
Páscoa, Catarina Cardoso
Turel, Iztok
Frangež, Robert
author2_role author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv DQ - Departamento de Química
RUN
dc.contributor.author.fl_str_mv Trobec, Tomaž
Sepčić, Kristina
Žužek, Monika Cecilija
Kladnik, Jerneja
Podjed, Nina
Páscoa, Catarina Cardoso
Turel, Iztok
Frangež, Robert
dc.subject.por.fl_str_mv Carbonyl
Cholinesterase
Enzyme inhibition
Glutathione S-transferase
Organoruthenium complex
Pyrithione
β-diketone
Medicine (miscellaneous)
Biochemistry, Genetics and Molecular Biology(all)
SDG 3 - Good Health and Well-being
topic Carbonyl
Cholinesterase
Enzyme inhibition
Glutathione S-transferase
Organoruthenium complex
Pyrithione
β-diketone
Medicine (miscellaneous)
Biochemistry, Genetics and Molecular Biology(all)
SDG 3 - Good Health and Well-being
description P4-0053 P1-0207 P1-0175 51852 39077
publishDate 2021
dc.date.none.fl_str_mv 2021-09-16
2021-09-16T00:00:00Z
2022-08-01T22:26:00Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10362/142771
url http://hdl.handle.net/10362/142771
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 2227-9059
PURE: 45749929
https://doi.org/10.3390/biomedicines9091243
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.source.none.fl_str_mv reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron:RCAAP
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron_str RCAAP
institution RCAAP
reponame_str Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
collection Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository.name.fl_str_mv Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
repository.mail.fl_str_mv
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