Universidad de Burgos RIUBU Principal Default Universidad de Burgos RIUBU Principal Default
  • español
  • English
  • français
  • Deutsch
  • português (Brasil)
  • italiano
Universidad de Burgos RIUBU Principal Default
  • Ayuda
  • Contattaci
  • Manda Feedback
  • Acceso abierto
    • Archivar en RIUBU
    • Acuerdos editoriales para la publicación en acceso abierto
    • Controla tus derechos, facilita el acceso abierto
    • Sobre el acceso abierto y la UBU
    • español
    • English
    • français
    • Deutsch
    • português (Brasil)
    • italiano
    • español
    • English
    • français
    • Deutsch
    • português (Brasil)
    • italiano
    JavaScript is disabled for your browser. Some features of this site may not work without it.

    Ricerca

    Tutto RIUBUArchivi & CollezioniData di pubblicazioneAutoriTitoliSoggettiQuesta CollezioneData di pubblicazioneAutoriTitoliSoggetti

    My Account

    LoginRegistrazione

    Statistiche

    Ver Estadísticas de uso

    Compartir

    Mostra Item 
    •   RIUBU Home
    • E-Prints
    • Untitled
    • Untitled
    • Artículos TERMOCIN
    • Mostra Item
    •   RIUBU Home
    • E-Prints
    • Untitled
    • Untitled
    • Artículos TERMOCIN
    • Mostra Item

    Por favor, use este identificador para citar o enlazar este ítem: http://hdl.handle.net/10259/4798

    Título
    Role of Seroalbumin in the Cytotoxicity of cis-Dichloro Pt(II) Complexes with (N^N)-Donor Ligands Bearing Functionalized Tails
    Autor
    Pérez Arnáiz, CristinaAutoridad UBU Orcid
    Leal, Jorge .
    Busto Vázquez, NataliaAutoridad UBU Orcid
    Carrión, María C. .
    Rubio Antolin, Ana RosaAutoridad UBU Orcid
    Ortiz, Imanol .
    Barone, Giampaolo
    Díaz de Greñu Puertas, BorjaAutoridad UBU Orcid
    Santolaya, Javier
    Leal Villalba, José MaríaAutoridad UBU Orcid
    Vaquero Gutiérrez, MónicaAutoridad UBU Orcid
    Jalón, Félix A.
    Manzano, Blanca R. .
    García Ruiz, BegoñaAutoridad UBU Orcid
    Publicado en
    Inorganic chemistry, 2018, V. 57, n 10, p. 6124-6134
    Editorial
    American Chemical Society
    Fecha de publicación
    2018-05-21
    ISSN
    0020-1669
    DOI
    10.1021/acs.inorgchem.8b00713
    Abstract
    Given the potent anticancer properties of cisdiamminedichloroplatinum( II) and knowing its mode of action, we synthesized four new cis-[PtCl2(N^N)] organoplatinum complexes, two with N-substituted pbi ligands (pbiR = 1-R-2-(2-pyridyl)benzimidazole) (namely, 1 and 2) and two more with 4,4′-disubstituted bpy ligands (bpy = 2,2′-bipyridine) (namely, 3 and 4). We explored their cytotoxicity and ability to bind to deoxyguanosine monophosphate (dGMP), DNA, and albumin models. By 1H NMR and UV−vis spectroscopies, circular dichroism, agarose gel electrophoresis, differential scanning calorimetry measurements, and density functional theory calculations, we verified that only 3 can form aquacomplex species after dimethyl sulfoxide solvation; surprisingly, 1, 2, and 3 can bind covalently to DNA, whereas 4 can form a noncovalent complex. Interestingly, only complexes 1 and 4 exhibit good cytotoxicity against human ovarian carcinoma (HeLa) cell line, whereas 2 and 3 are inactive. Although lung carcinoma (A549) cells are more resistant to the four platinum complexes than HeLa cells, when the protein concentration in the extracellular media is lower, the cytotoxicity becomes substantially enhanced. By native electrophoresis of bovine seroalbumin (BSA) and inductively coupled plasma mass spectrometry uptake studies we bear out, on one hand, that 2 and 3 can interact strongly with BSA and its cellular uptake is negligible and, on the other hand, that 1 and 4 can interact with BSA only weakly, its cellular uptake being higher by several orders. These results point up the important role of the protein binding features on their biological activity and cellular uptake of cis-“PtCl2” derivatives. Our results are valuable in the future rational design of new platinum complexes with improved biological properties, as they expose the importance not only of their DNA binding abilities but also of additional factors such as protein binding.
    Materia
    Chemistry, Physical and theoretical
    Química física
    URI
    http://hdl.handle.net/10259/4798
    Versión del editor
    http://dx.doi.org/10.1021/acs.inorgchem.8b00713
    Aparece en las colecciones
    • Artículos TERMOCIN
    • Artículos TML
    Files in questo item
    Nombre:
    Perez-IC_2018.pdf
    Tamaño:
    1.644Mb
    Formato:
    Adobe PDF
    Thumbnail
    Mostra/Apri

    Métricas

    Citas

    Academic Search
    Ver estadísticas de uso

    Exportar

    RISMendeleyRefworksZotero
    • edm
    • marc
    • xoai
    • qdc
    • ore
    • ese
    • dim
    • uketd_dc
    • oai_dc
    • etdms
    • rdf
    • mods
    • mets
    • didl
    • premis
    Mostra tutti i dati dell'item