Anti-degenerative effect of Apigenin, Luteolin and Quercetin on human keratinocyte and chondrocyte cultures: SAR evaluation
Anti-degenerative effect of Apigenin, Luteolin and Quercetin on human keratinocyte and chondrocyte cultures: SAR evaluation
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DOI：
10.1055/s-0043-120662
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发表时间：
2018-03-01
期刊：
影响因子：
2.2
通讯作者：
Panico, Annamaria
中科院分区：
文献类型：
--
作者：
Crasci, Lucia;Cardile, Venera;Panico, Annamaria
背景炎症是血管组织对不同刺激的反应而发生的动态过程，导致细胞损伤和组织变性。活性氧和氮物种(ROS和RNS)和晚期糖基化终末产物(AGEs)在退行性组织过程的发生和发展中起着关键的中介作用。生物黄酮类化合物具有广泛的药理活性。方法比较芹菜素和木犀草素两种黄酮类化合物和一种黄酮醇类化合物的抗氧化、抗糖化和抗退化作用，以及它们的羟基排列方式。此外，我们还在NCTC 2544和软骨细胞培养上测定了类黄酮类化合物对NO和糖胺多糖水平的调节能力，以及抗变性能力指数。结果所有受试类黄酮类化合物都具有自由基清除剂(Roo中心点和NO中心点)和糖基化终末产物抑制剂的作用，与它们的BDE、IP和分子平面性一致。根据较低的BDE(74.54千卡/摩尔)和IP(174.44千卡/摩尔)，槲皮素具有较高的ORAC值(2.70+/-0.12ORAC单位)。木犀草素对NO(48.19+/-0.18%)和AGEs(60.06+/-0.52%)的抑制作用最强，3-羟基与C‘6碳原子之间的扭转角较小(16.3°)。它们的作用方式取决于官能团、生物底物和使用的浓度。在任何情况下，它都可以被认为是一种适合防止退化过程的产品。
Background Inflammation is a dynamic process that occur on vascularized tissue in response to different stimuli causing cell injury and tissue degeneration. Reactive oxygen and nitrogen species (ROS and RNS) and advanced glycation end products (AGEs) have a key mediatory role in the development and progression of degenerative tissue process. The bioflavonoids possess a broad-spectrum of pharmacological activities. Their capability is related to their chemical structure.Methods In this study we evaluated and compare antioxidant, anti-glycative and anti-degenerative actions of two flavones apigenin and luteolin and a flavonol quercetin, in function of their hydroxyl groups arrangement. Moreover we assay, on NCTC 2544 and chondrocytes cultures, the flavonoids capacity to modulate NO and glycosamminoglycans levels, index of antidegenerative capacity.Results All tested flavonoids act as free radicals scavengers (ROO center dot and NO center dot) and advanced glycation end products inhibitors, in agreement with their BDE, IP and molecular planarity. Quercetin showed a high ORAC value (2.70 +/- 0.12 ORAC Units), according to a low BDE (74.54 Kcal/mol) and IP (174.44 Kcal/mol) values. Luteolin is the most active compound in the NO (48.19 +/- 0.18 %) and AGEs (60.06 +/- 0.52 %) inhibition, in function of a low torsion angle (16.3 degrees) between the 3-OH moiety and C' 6 carbon atom.Conclusion All tested flavonoids posses a protective role on degenerative tissue events. They acts in different manner depending on the functional groups, the biological substrate and the concentration used. In any case, it can be considered a suitable product preventing a degenerative processes.