RT Journal Article
T1 Gold(I) metallocyclophosphazenes with antibacterial potency and antitumor efficacy. Synergistic antibacterial action of a heterometallic gold and silver-cyclophosphazene
A1 Gascón, Elena
A1 Otal, Isabel
A1 Maisanaba, Sara
A1 Llana Ruíz-Cabello, María
A1 Valero Blanco, Eva María
A1 Repetto, Guillermo
A1 Jones, Peter G
A1 Oriol, Luis
A1 Jiménez, Josefina
K1 Phosphazenes
K1 Gold
K1 Antibacterial potency
K1 Antitumor efficacy
K1 Silver
AB One of the most important uses of phosphazenes today involves its biomedical applications. They can also be employed as scaffolds for the design and construction of a variety of ligands in order to coordinate them to metallic drugs. The coordination chemistry of the (amino)cyclotriphosphazene ligand, [N3P3(NHCy)6], towards gold(I) complexes has been studied. Neutral complexes, [N3P3(NHCy)6{AuX}n] (X = Cl or C6F5; n = 1 or 2) (1–4), cationic complexes, [N3P3(NHCy)6{Au(PR3)}n](NO3)n (PR3 = PPh3, PPh2Me, TPA; n = 1, 2 or 3) (6–12) [TPA = 1,3,5-triaza-7-phosphaadamantane] and a heterometallic compound [N3P3(NHCy)6{Au(PPh3)}2{Ag(PPh3)}] (NO3)3 (13) have been obtained and characterized by various methods including single-crystal X-ray diffraction for 7, which confirms the coordination of gold atoms to the nitrogens of the phosphazene ring. Compounds 1, 4, 6–13 were screened for in vitro cytotoxic activity against two tumor human cell lines, MCF7 (breast adenocarcinoma) and HepG2 (hepatocellular carcinoma), and for antimicrobial activity against five bacterial species including Gram-positive, Gram-negative, and Mycobacteria. Both the median inhibitory concentration (IC50) and minimum inhibitory concentration (MIC) values are among the lowest found for any gold or silver derivatives against the cell lines and particularly against the Gram-positive (S. aureus) strain and the mycobacteria used in this work. Structure–activity relationships are discussed in order to determine the influence of ancillary ligands and the number and type of metal atoms (silver or gold). Compounds 4 and 8 showed not only maximal potency on human cells but also some tumour selectivity. Remarkably, compound 13, with both gold and silver atoms, showed outstanding activity against both Gram-positive and Gram-negative strains (nanomolar range), thus having a cooperative effect between gold and silver, with MIC values which are similar or lower than those of gentamicine, ciprofloxacin and rifampicine. The broad spectrum antimicrobial efficacy of all these metallophosphazenes and particularly of heterometallic compound 13 could be very useful to obtain materials for surfaces with antimicrobial properties that are increasingly in demand.
PB Royal Society of Chemistry
YR 2022
FD 2022-08-22
LK https://hdl.handle.net/10433/19724
UL https://hdl.handle.net/10433/19724
LA en
NO Dalton Trans., 2022, 51, 13657
NO Proyectos de investigaciónMinisterio de Economia y Competitividad (MINECO)-FEDER, Spain, under the project grant number MAT2017-84838-PGobierno de Aragón-FEDER (Groups E47_20R and B25_20R, FEDER 2014-2020 “Construyendo Europa desde Aragón”) and by the European Regional Development Fund (FEDER)
NO Departamento de Química Inorgánica, Facultad de Ciencias, Instituto de Síntesis Química y Catálisis Homogénea (ISQCH), Universidad de Zaragoza-C.S.I.C
NO Departamento de Biología Molecular e Ingeniería Bioquímica, Área de Toxicología, Universidad Pablo de Olavide
NO Grupo de Genética de Micobacterias, Departamento de Microbiología, Pediatría, Radiología y Salud Pública, Universidad de Zaragoza,
NO Institut für Anorganische und Analytische Chemie, Technische Universität Braunschweig, Hagenring 30, D-38106 Braunschweig, Germany
NO Departamento de Química Orgánica, Instituto de Nanociencia y Materiales de Aragón-Facultad de Ciencias, Universidad de Zaragoza-C.S.I.C.
DS RIO
RD Jun 10, 2026