117605 20230519145530.0 doi 10.3390/biomedicines9121848 sideral 126990 ART-2021-126990 eng Quero J. Gold(I) complexes bearing alkylated 1, 3, 5-triaza-7-phosphaadamantane ligands as thermoresponsive anticancer agents in human colon cells 2021 Access copy available to the general public Unrestricted Overheating can affect solubility or lipophilicity, among other properties, of some an-ticancer drugs. These temperature-dependent changes can improve efficiency and selectivity of the drugs, since they may affect their bioavailability, diffusion through cell membrane or activity. One recent approach to create thermosensitive molecules is the incorporation of fluorine atoms in the chemical structure, since fluor can tune some chemical properties such as binding affinity. Herein we report the anticancer effect of gold derivatives with phosphanes derived from 1, 3, 5-triaza-7-phosphaadamantane (PTA) with long hydrocarbon chains and the homologous fluorinated chains. Besides, we analysed the influence of temperature in the cytotoxic effect. The studied gold(I) complexes with phosphanes derived from PTA showed antiproliferative effect on human colon carcinoma cells (Caco-2/TC7 cell line), probably by inhibiting cellular TrxR causing a dysfunction in the intracellular redox state. In addition, the cell cycle was altered by the activation of p53, and the complexes produce apoptosis through mitochondrial depolarization and the consequent activation of caspase-3. Furthermore, the results suggest that this cytotoxic effect is enhanced by hyperthermia and the presence of polyfluorinated chains. © 2021 by the authors. Licensee MDPI, Basel, Switzerland. info:eu-repo/grantAgreement/ES/CIBERObn/CB06-03-1012 info:eu-repo/grantAgreement/ES/DGA-FSE/B16-20R info:eu-repo/grantAgreement/ES/DGA-FSE/E07-20R info:eu-repo/grantAgreement/ES/MCIU/RED2018-102471-T info:eu-repo/grantAgreement/ES/MICINN-ISCIIII-FEDER/PID2019-104915RB-I00 info:eu-repo/grantAgreement/ES/MICINN/PID2019-104379RB-C21 info:eu-repo/semantics/openAccess by http://creativecommons.org/licenses/by/3.0/es/ 4.757 2021 BIOCHEMISTRY & MOLECULAR BIOLOGY 121 / 297 = 0.407 2021 Q2 T2 PHARMACOLOGY & PHARMACY 87 / 279 = 0.312 2021 Q2 T1 MEDICINE, RESEARCH & EXPERIMENTAL 62 / 140 = 0.443 2021 Q2 T2 0.874 2021 Medicine (miscellaneous) 2021 Q1 Biochemistry, Genetics and Molecular Biology (miscellaneous) 2021 Q1 3.0 2021 info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion Ruighi F. Osada J. Universidad de Zaragoza (orcid)0000-0002-8251-8457 Gimeno M.C. (orcid)0000-0003-0553-0695 Cerrada E. Universidad de Zaragoza (orcid)0000-0003-2457-3674 Rodriguez-Yoldi M.J. Universidad de Zaragoza (orcid)0000-0002-3595-7668 2010 760 Universidad de Zaragoza Dpto. Química Inorgánica Área Química Inorgánica 1012 410 Universidad de Zaragoza Dpto. Farmac.Fisiol.y Med.L.F. Área Fisiología 1002 060 Universidad de Zaragoza Dpto. Bioq.Biolog.Mol. Celular Área Bioquímica y Biolog.Mole. 9, 12 (2021), 1848 Biomedicines 2227-9059 3352461 http://zaguan.unizar.es/record/117605/files/texto_completo.pdf Versión publicada 2780010 http://zaguan.unizar.es/record/117605/files/texto_completo.jpg?subformat=icon icon Versión publicada oai:zaguan.unizar.es:117605 articulos driver 2023-05-18-15:30:01 ARTICLE