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991.
Aquaporins (AQPs) are membrane water/glycerol channels that are involved in many physiological functions. Aquaporin‐based modulators are predicted to have potential utility in the treatment of several diseases, as well as chemical tools to assess AQPs function in biological systems. We recently reported gold(III) compounds as human AQP3 inhibitors, with Auphen as the most potent of the series. In this work, we assessed the modulation of aquaporin‐7 (AQP7) expressed in an adipocyte cell model and show that Auphen significantly inhibits mouse and human AQP7. By homology modeling and molecular docking it was possible to identify the thioether groups of methionine residues, in particular Met47, as likely candidates for binding to the gold(III) complex. Our data point to Auphen as a useful chemical tool to detect AQP7 function. It might constitute a basis to develop inhibitors with improved affinity towards different aquaglyceroporin isoforms.  相似文献   
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The level of eleven target phenolic compounds was evaluated in dry fermented sausages added with vegetable extracts. Grape seed (GSE1 and GSE2) and cocoa extracts, rich in phenolic compounds, were added in the formulation of dry fermented sausages (“salchichón” and “fuet”). Evolution of the major monomeric and oligomeric phenolic compounds of these extracts was evaluated during sausage shelf life by UHPLC-MS/MS. Kind of sausage did not affect significantly overall stability of the target compounds. At the end of the ageing process, catechin and epicatechin were at 54–61%, gallic acid and galloylated flavan-3-ols at 59–91%, oligomeric flavan-3-ols at 72–95% and glycosylated flavonols at 56–88% (in cocoa treatment) and 82–94% (in GSE treatment) of the contents that were added to the meat batter. All phenolic compounds levels did not decrease further significantly after ageing until the end of shelf life. Sensory analyses showed no important differences between control and cocoa added products, while grape seed addition gave these products abnormal sensory profiles. The 0.5% (w/w) addition of vegetal extracts was suitable to enrich dry fermented sausages with health-beneficial polyphenols.  相似文献   
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Bulletin of Engineering Geology and the Environment - Weathering processes cause significant changes in the engineering properties of rocks. Slope instability in flysch rock formations along the...  相似文献   
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Dietary fibre has been employed as a sucrose and fat replacement in chocolates and can influence the physical and sensory characteristics of the resulting product. Formulations of sucrose‐free chocolates were developed with the addition of inulin and β‐glucan concentrate as partial substitutes for cocoa butter using a mixture design. The effects of the combinations of the three ingredients provided for the design on the texture, microstructure and sensory acceptance of the chocolates were investigated. The substitution of cocoa butter for inulin or β‐glucan concentrate decreased the hardness of the chocolates. It was possible to replace 10 g of cocoa butter in a 100‐g control formulation with inulin and still maintain good acceptance, while this same substitution with β‐glucan resulted in less acceptable chocolate, with a mean score of 6.4 on a scale from 0 to 10. Scanning electron microscopy (SEM) was used to investigate the effects of fibre addition by observing the developed microstructure.  相似文献   
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