RESUMEN
Platinum(II) complexes [Pt(4â³-fpbpy)Cl(2)] (1), [Pt(4â³-mepbpy)Cl(2)] (2), [Pt(4â³-mpbpy)Cl(2)] (3) and [Pt(4â³-bopbpy)Cl(2)] (4) {where 4â³-fpbpy=4-(4â³-fluorophenyl)-6-phenyl-2,2'-bipyridine, 4â³-mepbpy=4-(4â³-methylphenyl)-6-phenyl-2,2'-bipyridine, 4â³-mpbpy=4-(4â³-methoxyphenyl)-6-phenyl-2,2'-bipyridine, 4â³-bopbpy=4-(4â³-benzyloxyphenyl)-6-phenyl-2,2'-bipyridine} have been synthesized and characterized. The binding strength and binding mode of the complexes with HS DNA (Herring Sperm) have been investigated by absorption titration and viscosity measurement studies. The results have been revealed that the complexes bind to DNA by covalent mode with intrinsic binding constant K(b) ranging from 6.05×10(4)M(-1) to 3.48×10(5)M(-1). The unwinding angle of pUC19 DNA has been evaluated by gel electrophoresis assay. The brine shrimp bioassay has been performed to study the in vitro cytotoxic properties of the synthesized metal complexes.
Asunto(s)
2,2'-Dipiridil/análogos & derivados , Cisplatino/metabolismo , Cisplatino/farmacología , ADN/metabolismo , 2,2'-Dipiridil/síntesis química , 2,2'-Dipiridil/química , Absorción , Animales , Artemia/citología , Artemia/efectos de los fármacos , Bioensayo , Muerte Celular/efectos de los fármacos , Electrones , Fenómenos Magnéticos , Conformación de Ácido Nucleico , Plásmidos/química , Análisis Espectral , Termogravimetría , Volumetría , Viscosidad/efectos de los fármacosRESUMEN
An octahedral complexes of ruthenium with 2,9-dimethyl-1,10-phenanthroline (dmphen) and substituted terpyridine have been synthesized. The Ru(II) complexes have been characterized by elemental analyses, thermogravimetric analyses, magnetic moment measurements, FT-IR, electronic, (1)H NMR and FAB mass spectra. The binding strength and mode of interaction of the complexes with Herring Sperm DNA has been investigated using absorption titration and viscosity measurement studies. Results suggest that the substituent on terpyridine ligand affects the binding mode and binding ability of the complexes. Effect of time and ionic strength on DNA cleavage ability of complex has also been studied by gel electrophoresis. Results suggest that more than 200 mM concentration of NaCl decreases the cleavage ability of complex.
Asunto(s)
ADN/metabolismo , Compuestos Organometálicos/metabolismo , Piridinas/química , Rutenio/metabolismo , Absorción , Animales , ADN Circular/metabolismo , ADN Superhelicoidal/metabolismo , Electrones , Electroforesis en Gel de Agar , Cinética , Fenómenos Magnéticos , Espectroscopía de Resonancia Magnética , Masculino , Compuestos Organometálicos/síntesis química , Compuestos Organometálicos/química , Concentración Osmolar , Piridinas/síntesis química , Rutenio/química , Espectrofotometría Infrarroja , Espermatozoides/metabolismo , Termogravimetría , Factores de Tiempo , ViscosidadRESUMEN
Polypyridyl chlororuthenium(II) complexes have been synthesized and characterized. The binding mode of the complexes to DNA has been evaluated from the combined results of electronic absorption spectroscopy and viscosity measurement study. The results suggest that complexes 1, 2 and 3 bind to DNA via classical intercalation, electrostatic interaction and partial intercalation mode, respectively. Complex 2 shows less affinity for DNA. Cleavage of pUC19 DNA by complexes has been checked using gel electrophoresis. The data disclose that complex 1 has the highest cleaving ability.
Asunto(s)
ADN/metabolismo , Compuestos Organometálicos/química , Compuestos Organometálicos/síntesis química , Piridinas/química , Rutenio/química , Animales , ADN/química , Electroforesis en Gel de Agar , Masculino , Estructura Molecular , Compuestos Organometálicos/metabolismo , Espectrofotometría Atómica , Espermatozoides/química , Electricidad EstáticaRESUMEN
The copper(II) complexes of the type [Cu(SPF)(A(n))Cl]/[Cu(PFL)(A(n))Cl] (where SPF is sparfloxacin, PFL is pefloxacin and A(n) is 2,2'-dipyridylamine/pyridine-2-carboxalehyde/thiophene-2-carboxaldehyde) were synthesised and were found to have a pyramidal geometry with a square base. The superoxide dismutase (SOD) like activity of the complexes were measured using an NBT/NADH/PMS system, these were expressed in terms of the concentration of complex which termianates the formation of formazan by 50% (IC50 value) and found to range from 0.781 to 1.354 µM. The interactions of the complexes with DNA were studied by absorption titration, viscosity measurement and gel electrophoresis under physiological conditions. The antimicrobial efficiency of the complexes were tested on five different microorganisms and showed good biological activity.
Asunto(s)
Antiinfecciosos/química , Antiinfecciosos/farmacología , Bacterias/efectos de los fármacos , Cobre/química , Fluoroquinolonas/química , Fluoroquinolonas/farmacología , Superóxido Dismutasa , 2,2'-Dipiridil/análogos & derivados , 2,2'-Dipiridil/síntesis química , 2,2'-Dipiridil/química , Aldehídos/síntesis química , Aldehídos/química , Antiinfecciosos/síntesis química , ADN/química , Electroforesis en Gel de Agar , Fluoroquinolonas/síntesis química , Ligandos , Pruebas de Sensibilidad Microbiana , Compuestos Organometálicos/síntesis química , Compuestos Organometálicos/química , Compuestos Organometálicos/farmacología , Pefloxacina/síntesis química , Pefloxacina/química , Superóxido Dismutasa/metabolismo , Tiofenos/síntesis química , Tiofenos/químicaRESUMEN
Coordination of neutral bidentate ligand to copper ion in combination with gatifloxacin have been focused in this article. The effect of complexation reflects antibacterial activity, DNA interaction and SOD mimic activity of individual greatly. The geometry at the central metal ion provides a site for binding of superoxide anion responsible for better SOD mimic behaviour.
Asunto(s)
Antiinfecciosos/química , Antiinfecciosos/farmacología , Cobre/química , Cobre/farmacología , Fluoroquinolonas/química , Fluoroquinolonas/farmacología , Bacterias/efectos de los fármacos , ADN/metabolismo , Gatifloxacina , Pruebas de Sensibilidad Microbiana , Modelos Moleculares , Espectrofotometría , Espectrofotometría Infrarroja , Superóxidos/metabolismoRESUMEN
Here in we tried to increase an antibacterial activity of ciprofloxacin drug due to formation of mixed-ligand complexes. Synthesized compounds were found to be more potent compare to drugs, ligands and metal salt against selective gram((+ve)) and gram((-ve)) organisms. Interaction of the complexes with nucleic acid (DNA) were investigated using spectroscopic technique, viscosity measurement and gel electrophoresis and it was found that the complexes bind to DNA via intercalative mode.