Experimental Modeling of Flavonoid-Biomembrane Interactions.
Experimental Modeling of Flavonoid-Biomembrane Interactions.
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DOI：
10.1021/acs.langmuir.6b02219
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发表时间：
2016-11
期刊：
影响因子：
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通讯作者：
D. Sanver;B. Murray;A. Sadeghpour;M. Rappolt;A. Nelson
中科院分区：
文献类型：
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作者：
D. Sanver;B. Murray;A. Sadeghpour;M. Rappolt;A. Nelson
类黄酮与脂质的非特异性相互作用可以改变膜的特征（例如，厚度和波动）以及影响它们的治疗潜力。然而，关于类黄酮如何与脂质成分相互作用的细节知之甚少。用快速循环伏安法（RCV）研究了多种黄酮类化合物与磷脂在汞膜电极上的相互作用。数据显示，黄酮类化合物采用平面配置改变膜性能比非平面黄酮类化合物更显着。选择槲皮素、芦丁和替乌苷进行朗缪尔单分子膜、布鲁斯特角显微镜（BAM）和小角X射线散射（SAXS）的后续实验。在DOPC单层和BAM的表面可视化的松弛现象揭示了一个显着的单层稳定效果与槲皮素和tiliroside，而芦丁破坏的单层结构，使表面完全光滑。SAXS表明，单调的膜变薄与膜的平均波动的增加研究的所有化合物。大黄素、槲皮素和铁线蕨苷在6mol%时分别使DOPC的双层厚度降低了0.45、0.8和1.1 μ m。除了新奇的使用脂质单分子膜系统地表征各种黄酮类化合物的结构-活性关系（SAR），这是第一次报告调查tiliroside与仿生膜模型的效果。所有的类黄酮研究被认为是本地化的脂质/水界面区域。这两个本地化和膜扰动有其治疗活性的影响。
Nonspecific interactions of flavonoids with lipids can alter the membrane's features (e.g., thickness and fluctuations) as well as influence their therapeutic potentials. However, relatively little is known about the details of how flavonoids interact with lipid components. Structure-dependent interactions of a variety of flavonoids with phospholipid monolayers on a mercury (Hg) film electrode were established by rapid cyclic voltammetry (RCV). The data revealed that flavonoids adopting a planar configuration altered the membrane properties more significantly than nonplanar flavonoids. Quercetin, rutin, and tiliroside were selected for follow-up experiments with Langmuir monolayers, Brewster angle microscopy (BAM), and small-angle X-ray scattering (SAXS). Relaxation phenomena in DOPC monolayers and visualization of the surface with BAM revealed a pronounced monolayer stabilization effect with both quercetin and tiliroside, whereas rutin disrupted the monolayer structure rendering the surface entirely smooth. SAXS showed a monotonous membrane thinning for all compounds studied associated with an increase in the mean fluctuations of the membrane. Rutin, quercetin, and tiliroside decreased the bilayer thickness of DOPC by ∼0.45, 0.8, and 1.1 Å at 6 mol %, respectively. In addition to the novelty of using lipid monolayers to systematically characterize the structure-activity relationship (SAR) of a variety of flavonoids, this is the first report investigating the effect of tiliroside with biomimetic membrane models. All the flavonoids studied are believed to be localized in the lipid/water interface region. Both this localization and the membrane perturbations have implications for their therapeutic activity.