Afficher la notice abrégée

dc.contributor.authorGuarra, Federica
dc.contributor.authorBusto Vázquez, Natalia 
dc.contributor.authorGuerri, Annalisa
dc.contributor.authorMarchetti, Lorella
dc.contributor.authorMarzo, Tiziano
dc.contributor.authorGarcía Ruiz, Begoña 
dc.contributor.authorBiver, Tarita
dc.contributor.authorGabbiani, Chiara
dc.date.accessioned2020-06-10T12:29:12Z
dc.date.available2020-06-10T12:29:12Z
dc.date.issued2020-04
dc.identifier.issn0162-0134
dc.identifier.urihttp://hdl.handle.net/10259/5340
dc.description.abstractA silver(I) and a gold(I) complex of the fluorescent N-heterocyclic carbenic (NHC) ligand 1-(9-anthracenylmethyl)-3-(3-trimethylsilyl-2-propynil)-benzimidazol-2-ylidene have been synthesized and characterized. These compounds show cytotoxicity in the micromolar range and higher antiproliferative properties than cisplatin (CDDP) against several tumour cell lines such as SW480 (colon), A549 (lung) and HepG2 (liver). Both metal complexes are successfully internalized by SW480 cells being the silver compound the most accumulated. Subsequently, they were evaluated as inhibitors of the selenoenzyme Thioredoxin reductase (TrxR) and as DNA binders. Fluorescence microscopy confirmed that both protein and DNA binding could be involved in the biological activity of the compounds. The silver carbene was the most effective enzyme inhibitor with an IC50 in the nanomolar range. Also, interaction studies with natural double stranded DNA highlight a strong stabilisation of the double helix after binding to the Ag(I) carbene, indicating its potential suitability as dual-targeting anticancer active molecule.en
dc.description.sponsorship“la Caixa” Foundation (LCF/PR/PR12/11070003), Ministerio de Ciencia Innovación y Universidades-FEDER (RTI2018-102040-B-100) and Junta de Castilla y León-FEDER (BU305P18).es
dc.format.mimetypeapplication/pdf
dc.language.isoenges
dc.publisherElsevieres
dc.relation.ispartofJournal of Inorganic Biochemistry. 2020, V. 205, 110998es
dc.rightsAttribution-NonCommercial-NoDerivatives 4.0 Internacional*
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/*
dc.subjectDual anticancer drugen
dc.subjectMetal carbene complexesen
dc.subjectThioredoxin reductaseen
dc.subjectAnthracenyl dyesen
dc.subjectDNA interactionsen
dc.subject.otherBioquímicaes
dc.subject.otherBiochemistryen
dc.titleCytotoxic Ag(I) and Au(I) NHC-carbenes bind DNA and show TrxR inhibitionen
dc.typeinfo:eu-repo/semantics/articlees
dc.rights.accessRightsinfo:eu-repo/semantics/openAccesses
dc.relation.publisherversionhttps://doi.org/10.1016/j.jinorgbio.2020.110998es
dc.identifier.doi10.1016/j.jinorgbio.2020.110998
dc.relation.projectIDinfo:eu-repo/grantAgreement/MICINN/RTI2018-102040-B-100
dc.relation.projectIDinfo:eu-repo/grantAgreement/JCyL/BU305P18
dc.relation.projectIDinfo:eu-repo/grantAgreement/FundaciónLaCaixa/LCF/PR/PR12/11070003
dc.journal.titleJournal of Inorganic Biochemistryes
dc.volume.number205es
dc.page.initial110998es
dc.type.hasVersioninfo:eu-repo/semantics/acceptedVersiones


Fichier(s) constituant ce document

Thumbnail

Ce document figure dans la(les) collection(s) suivante(s)

Afficher la notice abrégée