Université de Lorraine, CNRS, LCPM, F-54000 Nancy, France.
Metallomics. 2020 Aug 19;12(8):1220-1229. doi: 10.1039/d0mt00103a.
Reactive oxygen species (ROS) are major sources of oxidative stress playing prominent roles in the development of several pathologies including cardiovascular and neurodegenerative diseases or cancers. The presence of transition biometal ions, specifically copper and iron, induces ROS formation by catalyzing the reduction of molecular oxygen to superoxide anion (O2˙-), hydrogen peroxide (H2O2) and hydroxyl (HO˙) radical. To limit ROS production and their detrimental effects, we report on the synthesis, physicochemical studies and antioxidant assays of an innovative series of synthetic pentapeptides exhibiting a dual direct/indirect mode of action, both as iron(iii)-chelators and as radical scavengers. These combined effects lead to a drastic reduction of in vitro reactive oxygen species production up to 95% for the more reactive hydroxyl radical.
活性氧（ROS）是氧化应激的主要来源，在包括心血管和神经退行性疾病或癌症在内的几种病理学的发展中起着重要作用。过渡金属离子（特别是铜和铁）的存在通过催化分子氧还原为超氧阴离子（O2˙-）、过氧化氢（H2O2）和羟基（HO˙）自由基，诱导 ROS 的形成。为了限制 ROS 的产生及其有害影响，我们报告了一系列创新的合成五肽的合成、物理化学研究和抗氧化剂测定，这些五肽具有直接/间接双重作用模式，既是铁（iii）螯合剂，又是自由基清除剂。这些综合效应导致体外活性氧（ROS）的产生减少了 95%，对更具反应性的羟基自由基的减少更为明显。
