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Organogold(III) compounds as experimental anticancer agents: chemical and biological profiles.
Massai, Lara; Cirri, Damiano; Michelucci, Elena; Bartoli, Gianluca; Guerri, Annalisa; Cinellu, Maria A; Cocco, Fabio; Gabbiani, Chiara; Messori, Luigi.
Afiliación
  • Massai L; Department of Chemistry, University of Florence, Via Della Lastruccia 3, Sesto Fiorentino, 50019, Florence, Italy. lara.massai@unifi.it.
  • Cirri D; Department of Chemistry, University of Florence, Via Della Lastruccia 3, Sesto Fiorentino, 50019, Florence, Italy.
  • Michelucci E; Mass Spectrometry Center (CISM), University of Florence, Via U. Schiff 6, Sesto Fiorentino, 50019, Florence, Italy.
  • Bartoli G; Department of Experimental and Clinical Medicine, University of Florence, Viale GB Morgagni 50, 50134, Florence, Italy.
  • Guerri A; Department of Chemistry, University of Florence, Via Della Lastruccia 3, Sesto Fiorentino, 50019, Florence, Italy.
  • Cinellu MA; Department of Chemistry and Pharmacy, University of Sassari, Via Vienna 2, 07100, Sassari, Italy.
  • Cocco F; Department of Chemistry and Pharmacy, University of Sassari, Via Vienna 2, 07100, Sassari, Italy.
  • Gabbiani C; Department of Chemistry and Industrial Chemistry, University of Pisa, Via Moruzzi 13, 56124, Pisa, Italy.
  • Messori L; Department of Chemistry, University of Florence, Via Della Lastruccia 3, Sesto Fiorentino, 50019, Florence, Italy. luigi.messori@unifi.it.
Biometals ; 29(5): 863-72, 2016 10.
Article en En | MEDLINE | ID: mdl-27476157
In the last few years gold(III) complexes have attracted growing attention in the medicinal chemistry community as candidate anticancer agents. In particular some organogold(III) compounds manifested quite attractive pharmacological behaviors in preclinical studies. Here we compare the chemical and biological properties of the novel organogold(III) complex [Au(bipy(dmb)-H)(NH(CO)CH3)][PF6] (Aubipy(aa)) with those of its parent compounds [Au(bipy(dmb)-H)(OH)][PF6] (Aubipy(c)) and [Au2(bipy(dmb)-H)2)(µ-O)][PF6]2 (Au2bipy(c)), previously synthesized and characterized. The three study compounds were comparatively assessed for their antiproliferative actions against HCT-116 cancer cells, revealing moderate cytotoxic effects. Proapoptotic and cell cycle effects were also monitored. Afterward, to gain additional mechanistic insight, the three gold compounds were challenged against the model proteins HEWL, RNase A and cytochrome c and reactions investigated through UV-Vis and ESI-MS analysis. A peculiar and roughly invariant protein metalation profile emerges in the three cases consisting of protein binding of {Au(bipy(dmb)-H)} moieties. The implications of these results are discussed in the frame of current knowledge on anticancer gold compounds.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Compuestos Orgánicos de Oro / Antineoplásicos Límite: Humans Idioma: En Revista: Biometals Asunto de la revista: BIOQUIMICA Año: 2016 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Países Bajos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Compuestos Orgánicos de Oro / Antineoplásicos Límite: Humans Idioma: En Revista: Biometals Asunto de la revista: BIOQUIMICA Año: 2016 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Países Bajos