ИСТИНА

Mitochondria-targeted cationic plastoquinone derivatives (SkQs, e.g. SkQ1, SkQR1) and their analogs lacking plastoquinol moiety (C12TPP, C12R1) can pass through bilayer phospholipid membrane. Their cationic forms are accumulated in isolated mitochondria or in mitochondria of living cells, driven by membrane potential. These compounds were extensively tested in model lipid membranes, isolated mitochondria and in living human cells in culture. It was found that SkQs are antioxidants that quench reactive oxygen species (ROS) in mitochondria and mild uncouplers that mediate transmembrane proton transport by fatty acids. Both properties result in efficient prevention of oxidative stress and protection of mitochondria and cells from damage by ROS, making SkQs a promising drug candidate against pathologies caused by excess mitochondrial ROS generation. Recent discovery of SkQ1 antibacterial activity in concentrations not toxic to human cells opens a perspective for development of new antibiotics. Experiments on animals revealed that SkQ alleviates damage induced by ischemia-reperfusion injury, prevents autoimmune arthritis, suppresses the development of Alzheimer's disease signs, inhibits the development of ophthalmological disorders, including dry eye syndrome (DES), and has anti-inflammatory activity. The first SkQ-based drug (eye drops Visomitin) is already developed and registered in Russia. More than 1 mln samples of Visomitin were already sold by drugstores. Clinical studies of orally-administered drug is in progress. In our talk we shall summarize recent experimental data on SkQ effects in animals, results of clinical trials and future perspectives of mitochondria-targeted antioxidants as therapeutic compounds.