RESUMO
The fluorescence spectra of the porous silicon modified by water solutions of biologically active materials and materials of biological origin are recorded as well as the fluorescence spectra of the porous silicon modified by lecithin monolayers grown on the surface of water solutions of the biologically active materials. The analysis of the obtained spectra made it possible to conclude on the effect of the studied materials on the content of ROS.
Assuntos
Produtos Biológicos/química , Lecitinas/química , Espécies Reativas de Oxigênio/análise , Silício/química , Difenidramina/química , Técnicas Eletroquímicas , Fluorescência , Isoproterenol/química , Porosidade , Soluções , Espectrometria de Fluorescência , Propriedades de Superfície , Água/químicaRESUMO
Involvement of protein kinase CK2 (2.7.11.1) in modulation of live cells trans-plasma membrane electron transport was first discovered. Using human erythrocytes a decrease of plasma membrane redox system (PMRS) activity is shown under the action of specific protein kinase CK2 inhibitors. Using inhibitory analysis the activity regulation of human erythrocytes PMRS by Ca(2+)-dependent and Ca(2+)-independent mechanisms were investigated. It was shown that functional Ca(2+)-antagonists (nitrendipine and calmidazolium) significantly increased, and functional Ca(2+)-agonists to some extent reduced or did not affect the trans-plasma membrane electron transport in these cells.
Assuntos
Sinalização do Cálcio/fisiologia , Cálcio/metabolismo , Caseína Quinase II/metabolismo , Membrana Eritrocítica/enzimologia , Eritrócitos/enzimologia , Éster Metílico do Ácido 3-Piridinacarboxílico, 1,4-Di-Hidro-2,6-Dimetil-5-Nitro-4-(2-(Trifluormetil)fenil)/farmacologia , Calcimicina/farmacologia , Agonistas dos Canais de Cálcio/farmacologia , Bloqueadores dos Canais de Cálcio/farmacologia , Caseína Quinase II/antagonistas & inibidores , Células Cultivadas , Transporte de Elétrons/efeitos dos fármacos , Membrana Eritrocítica/efeitos dos fármacos , Eritrócitos/efeitos dos fármacos , Humanos , Imidazóis/farmacologia , Nitrendipino/farmacologia , Oxirredução , Inibidores de Proteínas Quinases/farmacologiaRESUMO
A series of 5-amino-1H-pyrazoles was synthesized and studied as inhibitors of furin. The most potent compound, 5-amino-4-acetylamino-3-(4-methylphenylamino)1H-pyrazole, was found to retard the activity of furin by mixed-type inhibition with K = 288 microM. These findings permit to plan new ways for chemical modifications of the 5-amino-1H-pyrazole structure and design more potent furin inhibitors of non-peptide nature.
