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1.
Int J Biol Macromol ; 163: 801-816, 2020 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-32652152

RESUMEN

In this study, the new N, N, O tridentate donor water soluble isoniazid based biopolymer Schiff base ligand and their Co (II), Cu (II), Zn (II) metal complexes were prepared. The compounds were designed for potential biological application such as antibacterial, antifungal, anti-inflammatory, total antioxidant, antidiabetic and DNA binding studies. The synthesized compounds were illuminated in different light sources of various spectra were used to explore the functional groups of Biopolymer derivatives. Thermal degradation, thermal stability and percentage of mass loss for the prepared compounds were investigated through thermo gravimetric and differential thermal (TGA-DTA) analyses. Crystalline structure of synthesized biopolymer derivatives were explored by X-ray diffraction (XRD) studies, the crystallinity of chitosan is gradually decreased after the Schiff base and complex formation. Surface morphology and structures of the prepared compounds were examined using SEM analysis. The magnetic moment and magnetism of the metal complexes were studied using Vibrating-sample magnetometer (VSM). Antidiabetic studies of Biopolymer Schiff base and metal complexes were carried out by α-amylose inhibitory method. DNA nuclease activities of synthesized metal complexes were investigated by Ultra-Violet (UV) and viscometry methods. The Cu (II) complexes showed better DNA binding results than Co (II) and Zn (II) complexes.


Asunto(s)
Quitosano/análogos & derivados , Cobalto/química , Complejos de Coordinación/química , Cobre/química , Isoniazida/química , Bases de Schiff/química , Zinc/química , Antibacterianos/química , Antibacterianos/farmacología , Antifúngicos/química , Antifúngicos/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Fenómenos Químicos , Técnicas de Química Sintética , Quitosano/química , Desoxirribonucleasas/química , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Ligandos , Porosidad , Solubilidad , Espectroscopía Infrarroja por Transformada de Fourier , Análisis Espectral , Termogravimetría , Difracción de Rayos X , alfa-Amilasas/química
2.
Bioorg Chem ; 73: 100-108, 2017 08.
Artículo en Inglés | MEDLINE | ID: mdl-28648922

RESUMEN

Two novel oxovanadium(IV) complexes [VOL1]SO4(1) and [VOL2]SO4(2) containing Knoevenagel condensate Schiff base ligand (L1/L2) have been synthesized and characterized by physical, spectral and analytical methods. These complexes are reported as ionic in nature on the basis of elemental composition and molar conductance, and possess square pyramidal geometry around the central metal ions. The binding interactions of (1) and (2) with calf thymus DNA (CT DNA) were explored by absorption spectrophotometric titration, cyclic voltammetry data and viscosity measurements. The calculated intrinsic binding constant values (Kb) for (1) and (2) obtained from UV-Vis absorption studies are 0.4×105 and 5.6×105 (M-1) respectively. These experimental results indicate that (1) and (2) are intercalative binders and avid binder to CT DNA with different affinities. These complexes exhibit significant oxidative cleavage of supercoiled plasmid (pUC18) DNA in the presence of activators. In particular, the in vitro antimicrobial efficacy of oxovanadium(IV) complexes reveal that they are more active than free ligands. Besides, the in vitro cytotoxic effect of the titled complexes were examined on a bundle of human tumor cell lines such as MCF-7 and HeLa cancerous cell lines by the MTT method. Interestingly, complex (2) exhibits more potent cytotoxic activity than the other complex and standard drug (cisplatin). The mode of cell death was assessed by Hoechst 33258 staining morphological studies.


Asunto(s)
Antineoplásicos/farmacología , Complejos de Coordinación/farmacología , Compuestos de Vanadio/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Apoptosis/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Complejos de Coordinación/síntesis química , Complejos de Coordinación/química , Relación Dosis-Respuesta a Droga , Evaluación Preclínica de Medicamentos , Ensayos de Selección de Medicamentos Antitumorales , Células HeLa , Humanos , Células MCF-7 , Estructura Molecular , Bases de Schiff/química , Bases de Schiff/farmacología , Relación Estructura-Actividad , Células Tumorales Cultivadas , Compuestos de Vanadio/química
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