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Oxidative stress (OS) is one of the leading pathogenic factors of neurodegenerative and vascular diseases of the brain. The development of OS leads to functional disorders in various structural components of the brain tissue, making it appropriate to use drugs with antioxidant action under these conditions. In this regard, design of new antioxidant drugs with neuroprotective effects is an urgent task. Among promising antioxidant compounds is a natural neuropeptide carnosine (β-alanyl-L-histidine), with a wide range of biological properties. In various experimental models of CNS diseases it has been shown that carnosine protects the brain from damage by preventing the development of OS in brain tissue and increasing the efficiency of the endogenous antioxidant system, and preserves motor activity and long-term memory in animals subjected to testing in the open field, hole dipping and Morris water maze tests. Overall, ongoing research is aimed at creating new promising drugs with a neuroprotective effect based on carnosine, characterized by the ability to cross the blood-brain barrier and demonstrate desired properties during targeted delivery to the brain.