Synthesis, properties, antitumor and antibacterial activity of new Pt(II) and Pd(II) complexes with 2,2'-dithiobis(benzothiazole) ligand.
Mono- and binuclear Pt(II) and Pd(II) complexes with 2,2'-dithiobis(benzothiazole) (DTBTA) ligand are reported. [Pt(DTBTA)(DMSO)Cl]Cl∙CHCl3(1) and [Pd2(µ-Cl)2(DTBTA)2]Cl2(2) have been synthesized and structurally characterized by elemental analysis, IR,1H and13C NMR spectroscopy, MS spectrometry and the content of platinum and palladium was determined using a flame atomic spectrometer. Two different coordination modes of 1 and 2 complexes were found; in both complexes, the coordination of Pt(II) and Pd(II) ions involves the N(3) atoms of the ligand but the binuclear complex 2, is a cis-chloro-bridged palladium complex. Evaluation of their in vitro antitumor activity against two human tumor cell lines human breast cancer (MCF-7) and hepatocellular carcinoma (HepG2); and their antimicrobial activity against Escherichia coli and Kokuria rhizophila was performed. Only complex 1 showed a dose- and time-dependent cytotoxic activity against the two tumor cell lines, associated to apoptosis and accumulation of treated cells in G0/G1 phase of cell cycle, while both 1 and 2 exhibited antimicrobial activity with complex 1 much more potent. The study on intracellular uptake in both MCF-7 and HepG2 cell lines revealed that only platinum of complex 1 is present inside the cells, suggesting a different mode of action of the two compounds. This was also in agreement with the results obtained for the antitumor and antibacterial activity.
Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università di Palermo, Viale delle Scienze pad. 16, Parco d'Orleans, 90128 Palermo, Italy. Electronic address: simona.rubino@unipa.it.
Simona
S
Rubino
Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università di Palermo, Viale delle Scienze pad. 16, Parco d'Orleans, 90128 Palermo, Italy.
Rosalia
R
Busà
Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università di Palermo, Viale delle Scienze pad. 16, Parco d'Orleans, 90128 Palermo, Italy.
Alessandro
A
Attanzio
Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università di Palermo, Viale delle Scienze pad. 16, Parco d'Orleans, 90128 Palermo, Italy.
Rosa
R
Alduina
Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università di Palermo, Viale delle Scienze pad. 16, Parco d'Orleans, 90128 Palermo, Italy.
Vita
V
Di Stefano
Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università di Palermo, Viale delle Scienze pad. 16, Parco d'Orleans, 90128 Palermo, Italy.
Maria Assunta
MA
Girasolo
Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università di Palermo, Viale delle Scienze pad. 16, Parco d'Orleans, 90128 Palermo, Italy.
Santino
S
Orecchio
Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università di Palermo, Viale delle Scienze pad. 16, Parco d'Orleans, 90128 Palermo, Italy.
Luisa
L
Tesoriere
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D052160:Benzothiazoles / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D004926:Escherichia coli / Q000187:drug effects; D006801:Humans; D008024:Ligands; D008826:Microbial Sensitivity Tests; D010165:Palladium / Q000737:chemistry* / Q000494:pharmacology*; D017671:Platinum Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013057:Spectrum Analysis
D000900:Anti-Bacterial Agents; D052160:Benzothiazoles; D008024:Ligands; D017671:Platinum Compounds; D010165:Palladium
Anticancer activity; Antimicrobial activity; Heterocyclic nitrogen ligand; Palladium complex; Platinum complex