The diet polyphenols are a secondary metabolites of plants able to act on inflammation process. Their anti-inflammatory activity is articulated through several mechanisms that are related to their antioxidative and radical scavengers properties. Our work is focused on a novel approach to inflammatory disease management, based on anti-glycative and matrix metalloproteinases (MMPs) inhibition effects, as a connected phenomena. To better understand these correlation, polyphenols Structure–Activity Relationship (SAR) studies were also reported. The antioxidant polyphenols inhibit the AGEs at different levels of the glycation process in the following ways: (1) prevention of Amadori adduct oxidation; (2) trapping reactive dycarbonyl compounds; (3) attenuation of receptor for AGEs (RAGE) expression. Moreover, several flavonoids with radical scavenging property showed also MMPs inhibition interact directly with MMPs or indirectly via radical scavengers and AGEs reduction. The essential polyphenols features involved in these mechanisms are C2-C3 double bond and number and position of hydroxyl, glycosyl and O-methyl groups. These factors induce a change in molecular planarity interfering with the hydrogen bond formation, electron delocalization and metal ion chelation. In particular, C2-C3 double bond improve the antioxidant and MMPs inhibition, while the hydroxylation, glycosylation and methylation induce a positive and negative correlation, respectively.

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天然抗氧化剂多酚对炎症的控制：抗糖化活性与金属蛋白酶抑制作用

饮食中的多酚是植物的次级代谢产物，能够在炎症过程中起作用。它们的抗炎活性是通过几种与其抗氧化和自由基清除剂特性有关的机制表达出来的。我们的工作集中在一种基于抗糖化作用和基质金属蛋白酶（MMPs）抑制作用的炎性疾病管理新方法上，这是一种相互联系的现象。为了更好地理解这些相关性，还报道了多酚结构-活性关系（SAR）研究。抗氧化剂多酚通过以下方式在糖基化过程的不同水平上抑制AGEs：（1）防止Amadori加合物氧化；（2）捕获反应性二羰基化合物；（3）衰减AGEs（RAGE）表达的受体。而且，几种具有自由基清除性能的类黄酮还显示MMP抑制作用与MMP直接相互作用或通过自由基清除剂和AGEs还原间接相互作用。这些机制涉及的基本多酚特征是C2-C3双键以及羟基，糖基和O-甲基的数量和位置。这些因素引起分子平面度的变化，干扰了氢键的形成，电子离域和金属离子螯合。特别是，C2-C3双键可改善抗氧化剂和MMPs的抑制作用，而羟基化，糖基化和甲基化分别引起正相关和负相关。这些机制涉及的基本多酚特征是C2-C3双键以及羟基，糖基和O-甲基的数量和位置。这些因素引起分子平面度的变化，干扰了氢键的形成，电子离域和金属离子螯合。特别是，C2-C3双键可改善抗氧化剂和MMPs的抑制作用，而羟基化，糖基化和甲基化分别引起正相关和负相关。这些机制涉及的基本多酚特征是C2-C3双键以及羟基，糖基和O-甲基的数量和位置。这些因素引起分子平面度的变化，干扰了氢键的形成，电子离域和金属离子螯合。特别是，C2-C3双键可改善抗氧化剂和MMPs的抑制作用，而羟基化，糖基化和甲基化分别引起正相关和负相关。