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1.
Bioorg Med Chem ; 19(23): 7063-9, 2011 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-22047804

RESUMEN

The in vitro influence of Keggin structure polyoxotungstates, 12-tungstosilicic acid, H(4)SiW(12)O(40) (WSiA) and 12-tungstophosphoric acid, H(3)PW(12)O(40) (WPA), and monomer Na(2)WO(4) × 2H(2)O on rat synaptic plasma membrane (SPM) Na(+)/K(+)-ATPase and E-NTPDase activity was studied, whereas the commercial porcine cerebral cortex Na(+)/K(+)-ATPase served as a reference. Dose-dependent Na(+)/K(+)-ATPase inhibition was obtained for all investigated compounds. Calculated IC(50) (10 min) values, in mol/l, for SPM/commercial Na(+)/K(+)-ATPase, were: 3.4 × 10(-6)/4.3 × 10(-6), 2.9 × 10(-6)/3.1 × 10(-6) and 1.3 × 10(-3)/1.5 × 10(-3) for WSiA, WPA and Na(2)WO(4) × 2H(2)O, respectively. In the case of E-NTPDase, increasing concentrations of WSiA and WPA induced its activity reduction, while Na(2)WO(4) × 2H(2)O did not noticeably affect the enzyme activity at all investigated concentrations (up to 1 × 10(-3)mol/l). IC(50) (10 min) values, obtained from the inhibition curves, were (in mol/l): 4.1 × 10(-6) for WSiA and 1.6 × 10(-6) for WPA. Monolacunary Keggin anion was found as the main active molecular species present under physiological conditions (in the enzyme assays, pH 7.4), for the both polyoxotungstates solutions (1 mmol/l), using Fourier transform infrared (FT-IR) and micro-Raman spectroscopy. Additionally, commercial porcine cerebral cortex Na(+)/K(+)-ATPase was exposed to the mixture of Na(2)WO(4) × 2H(2)O and WSiA at different concentrations. Additive inhibition effect was achieved for lower concentrations of Na(2)WO(4) × 2H(2)O/WSiA (≤ 1 × 10(-3)/4 × 10(-6) mol/l), while antagonistic effect was obtained for all higher concentrations of the inhibitors.


Asunto(s)
Apirasa/antagonistas & inhibidores , Ácidos Fosfóricos/farmacología , Ácido Silícico/farmacología , ATPasa Intercambiadora de Sodio-Potasio/antagonistas & inhibidores , Membranas Sinápticas/efectos de los fármacos , Membranas Sinápticas/enzimología , Compuestos de Tungsteno/farmacología , Animales , Antígenos CD/metabolismo , Apirasa/metabolismo , Inhibidores Enzimáticos/farmacología , Masculino , Modelos Moleculares , Ratas , Ratas Wistar , ATPasa Intercambiadora de Sodio-Potasio/metabolismo , Espectroscopía Infrarroja por Transformada de Fourier , Espectrometría Raman
2.
J Colloid Interface Sci ; 500: 30-43, 2017 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-28395161

RESUMEN

Electrochemically exfoliated graphene is functionalized graphene with potential application in biomedicine. Two most relevant biological features of this material are its electrical conductivity and excellent water dispersibility. In this study we have tried to establish the correlation between graphene structure and its antibacterial properties. The exfoliation process was performed in a two electrode-highly oriented pyrolytic graphite electrochemical cell. Solution of ammonium persulfate was used as an electrolyte. Exfoliated graphene sheets were dispersed in aqueous media and characterized by atomic force microscopy, scanning electron microscopy, Raman spectroscopy, Fourier transform infrared spectroscopy, X photoelectron spectroscopy, X-ray diffraction, electron paramagnetic resonance, zeta potential, contact angle measurements and surface energy. Antibacterial assays have shown lack of the significant antibacterial activity. Major effect on bacteria was slight change of bacteria morphology. Membrane remained intact despite significant change of chemical content of membrane components.

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