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    Por favor, use este identificador para citar o enlazar este ítem: http://hdl.handle.net/10259/5340

    Título
    Cytotoxic Ag(I) and Au(I) NHC-carbenes bind DNA and show TrxR inhibition
    Autor
    Guarra, Federica
    Busto Vázquez, NataliaAutoridad UBU Orcid
    Guerri, Annalisa
    Marchetti, Lorella
    Marzo, Tiziano
    García Ruiz, BegoñaAutoridad UBU Orcid
    Biver, Tarita
    Gabbiani, Chiara
    Publicado en
    Journal of Inorganic Biochemistry. 2020, V. 205, 110998
    Editorial
    Elsevier
    Fecha de publicación
    2020-04
    ISSN
    0162-0134
    DOI
    10.1016/j.jinorgbio.2020.110998
    Zusammenfassung
    A 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.
    Palabras clave
    Dual anticancer drug
    Metal carbene complexes
    Thioredoxin reductase
    Anthracenyl dyes
    DNA interactions
    Materia
    Bioquímica
    Biochemistry
    URI
    http://hdl.handle.net/10259/5340
    Versión del editor
    https://doi.org/10.1016/j.jinorgbio.2020.110998
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    Documento(s) sujeto(s) a una licencia Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 Internacional
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    Guarra-jib_2020.pdf
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