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一种用于筛选多酚锌离子载体活性的简单脂质体测定法。

A simple liposome assay for the screening of zinc ionophore activity of polyphenols.

作者信息

Clergeaud Gael, Dabbagh-Bazarbachi Husam, Ortiz Mayreli, Fernández-Larrea Juan B, O'Sullivan Ciara K

机构信息

Nanobiotechnology & Bioanalysis Group, Department of Chemical Engineering, Universitat Rovira i Virgili, 43007 Tarragona, Spain.

Department of Biochemistry and Biotechnology, Universitat Rovira i Virgili, 43007 Tarragona, Spain.

出版信息

Food Chem. 2016 Apr 15;197(Pt A):916-23. doi: 10.1016/j.foodchem.2015.11.057. Epub 2015 Nov 14.

Abstract

An efficient liposomal system for screening the zinc ionophore activity of a selected library consisting of the most relevant dietary polyphenols is presented. The zinc ionophore activity was demonstrated by exploring the use of zinc-specific fluorophore FluoZin-3 loaded liposomes as simple membrane tools that mimic the cell membrane. The zinc ionophore activity was demonstrated as the capacity of polyphenols to transport zinc cations across the liposome membrane and increase the zinc-specific fluorescence of the encapsulated fluorophore FluoZin-3. In addition, the zinc chelation strength of the polyphenols was also tested in a competition assay based on the fluorescence quenching of zinc-dependent fluorescence emitted by zinc-FluoZin-3 complex. Finally, the correlation between the chelation capacity and ionophore activity is demonstrated, thus underlining the sequestering or ionophoric activity that the phenolic compounds can display, thus, providing better knowledge of the importance of the structural conformation versus their biological activity. Furthermore, the assays developed can be used as tools for rapid, high-throughput screening of families of polyphenols towards different biometals.

摘要

本文介绍了一种高效的脂质体系统,用于筛选由最相关的膳食多酚组成的特定文库的锌离子载体活性。通过探索使用负载锌特异性荧光团FluoZin-3的脂质体作为模拟细胞膜的简单膜工具,证明了锌离子载体活性。锌离子载体活性表现为多酚将锌阳离子转运穿过脂质体膜并增加包封的荧光团FluoZin-3的锌特异性荧光的能力。此外,还基于锌-FluoZin-3复合物发射的锌依赖性荧光的荧光猝灭,在竞争试验中测试了多酚的锌螯合强度。最后,证明了螯合能力与离子载体活性之间的相关性,从而强调了酚类化合物可以表现出的螯合或离子载体活性,进而更好地了解结构构象与其生物活性的重要性。此外,所开发的测定法可作为快速、高通量筛选多酚家族对不同生物金属的工具。

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