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1.
Int J Mol Sci ; 19(1)2017 Dec 27.
Artigo em Inglês | MEDLINE | ID: mdl-29280948

RESUMO

V13K, a 26-residue peptide, has been shown to have strong antimicrobial activity, negligible hemolytic activity, and significant anticancer activity. In the present work, V13K was used as the framework to investigate the influence of helicity, as influenced by d-amino acid substitutions in the center of the peptide polar and non-polar faces of the amphipathic helix, on biological activity. The antibacterial and anticancer activities of the peptides were investigated. Atomic force microscopy and other biophysical methods were used to investigate the effect of peptide helicity on biological activity. The results showed the importance of suitable and rational modification of membrane-active peptides, based on helicity, in optimizing potential biological activity.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Peptídeos/química , Peptídeos/farmacologia , Sequência de Aminoácidos , Substituição de Aminoácidos , Antibacterianos/metabolismo , Antineoplásicos/metabolismo , Linhagem Celular Tumoral , Escherichia coli/efeitos dos fármacos , Infecções por Escherichia coli/tratamento farmacológico , Humanos , Interações Hidrofóbicas e Hidrofílicas , Testes de Sensibilidade Microbiana , Neoplasias/tratamento farmacológico , Peptídeos/genética , Estrutura Secundária de Proteína , Estereoisomerismo
2.
Sci Rep ; 6: 29145, 2016 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-27363513

RESUMO

In this study, to systematically investigate the targeting specificity of membrane-active peptides on different types of cell membranes, we evaluated the effects of peptides on different large unilamellar vesicles mimicking prokaryotic, normal eukaryotic, and cancer cell membranes by single-molecule force spectroscopy and spectrum technology. We revealed that cationic membrane-active peptides can exclusively target negatively charged prokaryotic and cancer cell model membranes rather than normal eukaryotic cell model membranes. Using Acholeplasma laidlawii, 3T3-L1, and HeLa cells to represent prokaryotic cells, normal eukaryotic cells, and cancer cells in atomic force microscopy experiments, respectively, we further studied that the single-molecule targeting interaction between peptides and biological membranes. Antimicrobial and anticancer activities of peptides exhibited strong correlations with the interaction probability determined by single-molecule force spectroscopy, which illustrates strong correlations of peptide biological activities and peptide hydrophobicity and charge. Peptide specificity significantly depends on the lipid compositions of different cell membranes, which validates the de novo design of peptide therapeutics against bacteria and cancers.


Assuntos
Peptídeos Catiônicos Antimicrobianos/química , Bicamadas Lipídicas/química , Neoplasias/tratamento farmacológico , Peptídeos/química , Sequência de Aminoácidos/efeitos dos fármacos , Sequência de Aminoácidos/genética , Células HeLa , Humanos , Microscopia de Força Atômica , Neoplasias/genética , Neoplasias/patologia , Peptídeos/farmacologia , Conformação Proteica em alfa-Hélice , Estrutura Secundária de Proteína , Imagem Individual de Molécula , Relação Estrutura-Atividade
3.
Sci Total Environ ; 569-570: 332-341, 2016 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-27344122

RESUMO

The transfer of nutrients from soil to runoff often causes unexpected pollution in water bodies. In this study, a mathematical model that relates to the detachment of soil particles by water flow and the degree of mixing between overland flow and soil nutrients was proposed. The model assumes that the mixing depth is an integral of average water flow depth, and it was evaluated by experiments with three water inflow rates to bare soil surfaces and to surfaces with eight treatments of different stone coverages. The model predicted outflow rates were compared with the experimentally observed data to test the accuracy of the infiltration parameters obtained by curve fitting the models to the data. Further analysis showed that the comprehensive mixing coefficient (ke) was linearly correlated with Reynolds' number Re (R(2)>0.9), and this relationship was verified by comparing the simulated potassium concentration and cumulative mass with observed data, respectively. The best performance with the bias error analysis (Nash Sutcliffe coefficient of efficiency (NS), relative error (RE) and the coefficient of determination (R(2))) showed that the predicted data by the proposed model was in good agreement with the measured data. Thus the model can be used to guide soil-water and fertilization management to minimize nutrient runoff from cropland.

4.
Sci Total Environ ; 557-558: 590-600, 2016 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-27037880

RESUMO

Nutrients transport is a main source of water pollution. Several models describing transport of soil nutrients such as potassium, phosphate and nitrate in runoff water have been developed. The objectives of this research were to describe the nutrients transport processes by considering the effect of rainfall detachment, and to evaluate the factors that have greatest influence on nutrients transport into runoff. In this study, an existing mass-conservation equation and rainfall detachment process were combined and augmented to predict runoff of nutrients in surface water in a Loess Plateau soil in Northwestern Yangling, China. The mixing depth is a function of time as a result of rainfall impact, not a constant as described in previous models. The new model was tested using two different sub-models of complete-mixing and incomplete-mixing. The complete-mixing model is more popular to use for its simplicity. It captured the runoff trends of those high adsorption nutrients, and of nutrients transport along steep slopes. While the incomplete-mixing model predicted well for the highest observed concentrations of the test nutrients. Parameters inversely estimated by the models were applied to simulate nutrients transport, results suggested that both models can be adopted to describe nutrients transport in runoff under the impact of rainfall.

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