Shchulkin A V
Pavlov Ryazan State Medical University, Ryazan, Russia.
Zh Nevrol Psikhiatr Im S S Korsakova. 2018;118(12. Vyp. 2):87-93. doi: 10.17116/jnevro201811812287.
The review article presents a modern concept of the mechanism of antioxidant and antihypoxic action of the original drug mexidol (2-ethyl-6-methyl-3-hydroxypyridine succinate). The direct antioxidant activity of mexidol has been described, which consists in the ability of the drug to inactivate free radicals and increase the activity of the antioxidant enzymes glutathione peroxidase and superoxide dismutase in vitro. The results of the indirect antioxidant activity of mexidol, manifested in the increased expression under the ischemia of the transcription factor Nrf2, responsible for the cell resistance to oxidative stress are presented. The antihypoxic action of mexidol due to the presence of succinic acid in its molecule, which on the one hand supports the work of the Krebs cycle succinate oxidase under oxygen deficiency conditions, and on the other hand, binds to its specific receptors (GPR91), and starts a cascade of biochemical reactions that increases the body's resistance to lack of oxygen is discussed. The results of preclinical and clinical studies confirming the antioxidant and antihypoxic effects of mexidol are summarized.
这篇综述文章介绍了原药美西多福（2-乙基-6-甲基-3-羟基吡啶琥珀酸盐）抗氧化和抗缺氧作用机制的现代概念。文中描述了美西多福的直接抗氧化活性，即该药物在体外使自由基失活并提高抗氧化酶谷胱甘肽过氧化物酶和超氧化物歧化酶活性的能力。还介绍了美西多福间接抗氧化活性的结果，表现为在缺血状态下负责细胞对氧化应激抵抗的转录因子Nrf2表达增加。讨论了美西多福的抗缺氧作用，这是由于其分子中存在琥珀酸，一方面在缺氧条件下支持三羧酸循环琥珀酸氧化酶的工作，另一方面与特定受体（GPR91）结合，并启动一系列生化反应，从而增强机体对缺氧的耐受性。总结了证实美西多福抗氧化和抗缺氧作用的临床前和临床研究结果。
