An array of poly- and mononuclear complexes of Pt(II) with polypyridyl ligands is reported. The framework complexes [(PtCl2)2(bpp)2(l-PtCl2)](H2O)2 [bpp = 2,3-bis(2-pyridyl)pyrazine], [PtCl2(l-tptz)PtClNCPh]Cl [tptz = 2,4,6-tris(2-pyridyl)-1,3,5-triazine], and mononuclear PtCl2(NH2dpt) [NH2dpt = 4-amino-3,5-bis(2-pyridyl)-1,2,4-triazole] have been prepared and structurally characterized. Both neutral and ionic complexes are present, with bifunctional and monofunctional Pt(II) moieties, whose size and shape enable them to behave as novel scaffolds for DNA binding. Pt(II) complexes were tested for their biological activity. Cell viability assay and flow cytometric analysis demonstrated that these complexes, particularly [PtCl2(l-tptz)PtClNCPh]Cl, were effective death inducers in human colon rectal carcinoma HT29 cells and their cytotoxic activity was higher than that exerted by cisplatin. Morphological analysis of treated HT29 cells, performed by fluorescence microscopy after Hoechst 33258 staining, showed the appearance of the typical features of apoptosis. Moreover, our results suggested that mitochondria are involved in apoptosis induced by Pt(II) complexes in HT29 cells as demonstrated by dissipation of mitochondrial transmembrane potential.

RUBINO S, PORTANOVA P, ALBANESE A, CALVARUSO G, ORECCHIO S, FONTANA G, et al. (2007). MONO- AND POLYNUCLEAR COMPLEXES OF PT(II) WITH POLYPYRIDYL LIGANDS SYNTHESIS, SPECTROSCOPIC AND STRUCTURAL CHARACTERIZATION AND CYTOTOXIC ACTIVITY. JOURNAL OF INORGANIC BIOCHEMISTRY, 101(10), 1473-1482 [10.1016/j.jinorgbio.2007.06.024].

MONO- AND POLYNUCLEAR COMPLEXES OF PT(II) WITH POLYPYRIDYL LIGANDS SYNTHESIS, SPECTROSCOPIC AND STRUCTURAL CHARACTERIZATION AND CYTOTOXIC ACTIVITY

RUBINO, Simona;PORTANOVA, Patrizia;ALBANESE, Antonella;CALVARUSO, Giuseppe;ORECCHIO, Santino;FONTANA, Gianfranco;STOCCO, Giancarlo
2007-01-01

Abstract

An array of poly- and mononuclear complexes of Pt(II) with polypyridyl ligands is reported. The framework complexes [(PtCl2)2(bpp)2(l-PtCl2)](H2O)2 [bpp = 2,3-bis(2-pyridyl)pyrazine], [PtCl2(l-tptz)PtClNCPh]Cl [tptz = 2,4,6-tris(2-pyridyl)-1,3,5-triazine], and mononuclear PtCl2(NH2dpt) [NH2dpt = 4-amino-3,5-bis(2-pyridyl)-1,2,4-triazole] have been prepared and structurally characterized. Both neutral and ionic complexes are present, with bifunctional and monofunctional Pt(II) moieties, whose size and shape enable them to behave as novel scaffolds for DNA binding. Pt(II) complexes were tested for their biological activity. Cell viability assay and flow cytometric analysis demonstrated that these complexes, particularly [PtCl2(l-tptz)PtClNCPh]Cl, were effective death inducers in human colon rectal carcinoma HT29 cells and their cytotoxic activity was higher than that exerted by cisplatin. Morphological analysis of treated HT29 cells, performed by fluorescence microscopy after Hoechst 33258 staining, showed the appearance of the typical features of apoptosis. Moreover, our results suggested that mitochondria are involved in apoptosis induced by Pt(II) complexes in HT29 cells as demonstrated by dissipation of mitochondrial transmembrane potential.
2007
RUBINO S, PORTANOVA P, ALBANESE A, CALVARUSO G, ORECCHIO S, FONTANA G, et al. (2007). MONO- AND POLYNUCLEAR COMPLEXES OF PT(II) WITH POLYPYRIDYL LIGANDS SYNTHESIS, SPECTROSCOPIC AND STRUCTURAL CHARACTERIZATION AND CYTOTOXIC ACTIVITY. JOURNAL OF INORGANIC BIOCHEMISTRY, 101(10), 1473-1482 [10.1016/j.jinorgbio.2007.06.024].
File in questo prodotto:
File Dimensione Formato  
1-s2.0-S0162013407001511-main.pdf

Solo gestori archvio

Dimensione 1.07 MB
Formato Adobe PDF
1.07 MB Adobe PDF   Visualizza/Apri   Richiedi una copia

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/19004
Citazioni
  • ???jsp.display-item.citation.pmc??? 1
  • Scopus 34
  • ???jsp.display-item.citation.isi??? 31
social impact