A series of novel Ga(III)-pyridine carboxylates ([Ga(Pic)3]·H2O (GaPic; HPic = picolinic acid), H3O[Ga(Dpic)2]·H2O (GaDpic; H2Dpic = dipicolinic acid), [Ga(Chel)(H2O)(OH)]2·4H2O (GaChel; H2Chel = chelidamic acid) and [Ga(Cldpic)(H2O)(OH)]2 (GaCldpic; H2Cldpic = 4-chlorodipicolinic acid)) have been synthesized by simple one-step procedure. Vibrational spectroscopy (mid-IR), elemental analysis, thermogravimetric analysis and X-ray diffraction confirmed complexes molecular structure, inter and intramolecular interactions and their influence to spectral and thermal properties. Moreover, complex species speciation was described in Ga(III)-HPic and Ga(III)-H2Dpic systems by potentiometry and 1H NMR spectroscopy and mononuclear complex species were determined; [Ga(Pic)2]+ (logβ021 = 16.23(6)), [Ga(Pic)3] (logβ031 = 20.86(2)), [Ga(Dpic)2]- (logβ021 = 15.42(9)) and [Ga(Dpic)2(OH)]2- (logβ-121 = 11.08(4)). To confirm the complexes stability in 1% DMSO (primary solvent for biological testing), timescale 1H NMR spectra were measured (immediately after dissolution up to 96 h). Antimicrobial activity evaluated by IC50 (0.05 mM) is significant for GaDpic and GaCldpic against difficult to treat and multi-resistant P. aeruginosa. On the other hand, the GaPic complex is most effective against Jurkat, MDA-MB-231 and A2058 cancer cell lines and significantly also decreases the HepG2 cancer cells viability at 75 and 100 μM concentrations in a relatively short time (up to 48 h). In addition, fluorescence measurements have been used to elucidate bovine serum albumin binding activity between ligands, Ga(III) complexes and bovine serum albumin.

• Keywords
• Anticancer, Antimicrobial, BSA binding, Ga(III) complexes, Potentiometry, Stability,
• MeSH
• Cell Line MeSH
• Coordination Complexes * pharmacology   chemistry   MeSH
• Humans MeSH
• Ligands MeSH
• Molecular Structure MeSH
• Neoplasms * MeSH
• Pyridines pharmacology   MeSH
• Serum Albumin, Bovine metabolism   MeSH
• Check Tag
• Humans MeSH
• Publication type
• Journal Article MeSH
• Research Support, Non-U.S. Gov't MeSH
• Names of Substances
• Coordination Complexes * MeSH
• Ligands MeSH
• Pyridines MeSH
• Serum Albumin, Bovine MeSH

Three silver(I) dipeptide complexes [Ag(GlyGly)]n(NO3)n (AgGlyGly), [Ag2(GlyAla)(NO3)2]n (AgGlyAla) and [Ag2(HGlyAsp)(NO3)]n (AgGlyAsp) were prepared, investigated and characterized by vibrational spectroscopy (mid-IR), elemental and thermogravimetric analysis and mass spectrometry. For AgGlyGly, X-ray crystallography was also performed. Their stability in biological testing media was verified by time-dependent NMR measurements. Their in vitro antimicrobial activity was evaluated against selected pathogenic microorganisms. Moreover, the influence of silver(I) dipeptide complexes on microbial film formation was described. Further, the cytotoxicity of the complexes against selected cancer cells (BLM, MDA-MB-231, HeLa, HCT116, MCF-7 and Jurkat) and fibroblasts (BJ-5ta) using a colorimetric MTS assay was tested, and the selectivity index (SI) was identified. The mechanism of action of Ag(I) dipeptide complexes was elucidated and discussed by the study in terms of their binding affinity toward the CT DNA, the ability to cleave the DNA and the ability to influence numbers of cells within each cell cycle phase. The new silver(I) dipeptide complexes are able to bind into DNA by noncovalent interaction, and the topoisomerase I inhibition study showed that the studied complexes inhibit its activity at a concentration of 15 μM.

• Keywords
• DNA interaction, anticancer activity, antimicrobial activity, cell cycle arrest, crystal structure, dipeptide, silver(I) complexes, stability, topoisomerase I inhibition,
• MeSH
• Anti-Infective Agents chemical synthesis   chemistry   pharmacology   MeSH
• Cell Cycle drug effects   MeSH
• Chemical Phenomena MeSH
• Dipeptides chemistry   MeSH
• Coordination Complexes chemical synthesis   chemistry   pharmacology   MeSH
• Crystallography, X-Ray MeSH
• Humans MeSH
• Molecular Conformation MeSH
• Cell Line, Tumor MeSH
• Antineoplastic Agents chemical synthesis   chemistry   pharmacology   MeSH
• Molecular Dynamics Simulation MeSH
• Spectrum Analysis MeSH
• Drug Stability MeSH
• Silver chemistry   MeSH
• Chemistry Techniques, Synthetic MeSH
• Thermogravimetry MeSH
• Dose-Response Relationship, Drug MeSH
• Structure-Activity Relationship MeSH
• Check Tag
• Humans MeSH
• Publication type
• Journal Article MeSH
• Names of Substances
• Anti-Infective Agents MeSH
• Dipeptides MeSH
• Coordination Complexes MeSH
• Antineoplastic Agents MeSH
• Silver MeSH

Two silver(i) complexes, {[Ag7(2-pypo)3(NO3)]} n (1) and [Ag(3-pypoH)(3-pypoH2)] (2) (pypoH2 - pyridylphosphonic acid) were prepared and characterized by relevant methods in the solid state (elemental, spectral, thermal and structural analysis). Typical argentophilic interactions were observed in complex 1. The synthesized Ag(i) complexes were tested toward reduction to silver(0) using short wavelength UV-radiation and they revealed remarkable light-insensitivity in comparison to silver nitrate. SEM experiments were performed to observe the reduction of silver after the UV-light exposure of the samples. Light-insensitivity with the examined thermal stability and insolubility of the new complexes demonstrates their high potential to be used as light-insensitive materials in medical devices.

• Publication type
• Journal Article MeSH