Department of Applied Chemistry College of Science, China Agricultural University Haidian District, Beijing, 100089, China.
ChemMedChem. 2020 Mar 5;15(5):404-410. doi: 10.1002/cmdc.201900695. Epub 2020 Feb 11.
Mitochondrial oxidative damage and dysfunction contribute to a wide range of human diseases. Considering the limitation of conventional antioxidants and that mitochondria are the main source of reactive oxygen species (ROS) which induce oxidative damage, mitochondria-targeted antioxidants which can selectively block mitochondrial oxidative damage and prevent various types of cell death have been widely developed. As a lipophilic cation, triphenylphosphonium (TPP) has been commonly used in designing mitochondria-targeted antioxidants. Conjugated with the TPP moiety, antioxidants can achieve more than 1000-fold higher mitochondrial concentration depending on cell membrane potentials and mitochondrial membrane potentials. Herein we discuss the deficiencies of conventional antioxidants and the advantages of mitochondrial targeting, and review various types of TPP-based mitochondria-targeted antioxidants. These provide theoretical and background support for the design of new anti-oxidant.
线粒体氧化损伤和功能障碍与多种人类疾病有关。考虑到传统抗氧化剂的局限性，以及线粒体是产生诱导氧化损伤的活性氧 (ROS) 的主要来源，因此已经广泛开发了能够选择性阻断线粒体氧化损伤并预防各种类型细胞死亡的线粒体靶向抗氧化剂。作为一种亲脂性阳离子，三苯基膦（TPP）常用于设计线粒体靶向抗氧化剂。与 TPP 部分结合后，抗氧化剂可以根据细胞膜电位和线粒体膜电位达到 1000 倍以上的线粒体浓度。本文讨论了传统抗氧化剂的缺陷和线粒体靶向的优势，并综述了各种基于 TPP 的线粒体靶向抗氧化剂。这些为新型抗氧化剂的设计提供了理论和背景支持。
