Meleleo Daniela, Avato Pinarosa, Conforti Filomena, Argentieri Maria Pia, Messina Giovanni, Cibelli Giuseppe, Mallamaci Rosanna
Department of Science of Agriculture, Food, Natural Resources and Engineering, University of Foggia, 71122 Foggia, Italy.
Department of Pharmacy-Drug Sciences, University of Bari "Aldo Moro", 70125 Bari, Italy.
Membranes (Basel). 2023 Jun 14;13(6):600. doi: 10.3390/membranes13060600.
Flavonoids are specialized metabolites produced by plants, as free aglycones or as glycosylated derivatives, which are particularly endowed with a variety of beneficial health properties. The antioxidant, anti-inflammatory, antimicrobial, anticancer, antifungal, antiviral, anti-Alzheimer's, anti-obesity, antidiabetic, and antihypertensive effects of flavonoids are now known. These bioactive phytochemicals have been shown to act on different molecular targets in cells including the plasma membrane. Due to their polyhydroxylated structure, lipophilicity, and planar conformation, they can either bind at the bilayer interface or interact with the hydrophobic fatty acid tails of the membrane. The interaction of quercetin, cyanidin, and their -glucosides with planar lipid membranes (PLMs) similar in composition to those of the intestine was monitored using an electrophysiological approach. The obtained results show that the tested flavonoids interact with PLM and form conductive units. The modality of interaction with the lipids of the bilayer and the alteration of the biophysical parameters of PLMs induced by the tested substances provided information on their location in the membrane, helping to elucidate the mechanism of action which underlies some pharmacological properties of flavonoids. To our knowledge, the interaction of quercetin, cyanidin, and their -glucosides with PLM surrogates of the intestinal membrane has never been previously monitored.
黄酮类化合物是植物产生的特殊代谢产物，以游离苷元或糖基化衍生物的形式存在，尤其具有多种有益健康的特性。目前已知黄酮类化合物具有抗氧化、抗炎、抗菌、抗癌、抗真菌、抗病毒、抗阿尔茨海默病、抗肥胖、抗糖尿病和抗高血压作用。这些生物活性植物化学物质已被证明作用于细胞中的不同分子靶点，包括质膜。由于它们的多羟基化结构、亲脂性和平面构象，它们可以结合在双层界面处或与膜的疏水脂肪酸尾部相互作用。使用电生理方法监测了槲皮素、花青素及其β-糖苷与组成与肠道相似的平面脂质膜（PLM）的相互作用。所得结果表明，所测试的黄酮类化合物与PLM相互作用并形成导电单元。与双层脂质的相互作用方式以及所测试物质引起的PLM生物物理参数的改变提供了它们在膜中位置的信息，有助于阐明黄酮类化合物某些药理特性的作用机制。据我们所知，此前从未监测过槲皮素、花青素及其β-糖苷与肠膜PLM替代物的相互作用。
