Meldonium是一种具有已知抗心绞痛作用的物质,已被大量研究和人体临床试验证明;然而,它在欧盟范围内没有营销授权,只在前苏联共和国.自2016年以来,meldonium已被世界反兴奋剂机构(WADA)列入S4代谢调节剂清单。在表演运动员中,meldonium现在被认为是一种掺杂剂,由于其在运动期间和之后减少乳酸产生的能力,它增强糖原储存和利用的能力,及其对氧化应激的保护作用。一起,这些属性可以显著提高有氧耐力,心功能,和容量以及缩短恢复时间(允许更高强度的训练),从而提高性能。这篇综述的目的是强调meldonium对线粒体功能障碍(MD)的保护作用的最重要机制,负责氧化应激,炎症,和称为“运动心脏综合征”的心脏变化。“Meldonium充当γ-丁甜菜碱羟化酶(BBOX)的抑制剂,通过有机阳离子/肉碱转运蛋白2(OCTN2)防止肉碱的从头合成及其在肠道水平的吸收,并将脂肪酸的氧化引导到过氧化物酶体。脂肪酸的线粒体β-氧化的减少导致脂质过氧化产物的减少,脂质过氧化产物引起氧化应激并阻止与许多病理障碍有关的酰基/乙酰肉碱的形成。鉴于最近发现长时间高强度运动对心血管健康和冠状动脉粥样硬化的潜在有害影响,对于使用meldonium等物质作为运动员的保护性补充剂的理由,可能有合理的论据。
Meldonium is a substance with known anti-anginal effects demonstrated by numerous studies and human clinical trials; however, it does not possess marketing authorization within the European Union, only in ex-Soviet republics. Since 2016, meldonium has been included by the World Anti-doping Agency (WADA) on the S4 list of metabolic modulators. In performance athletes, meldonium is now considered a doping agent due to its capacity to decrease lactate production during and after exercise, its capability to enhance the storage and utilization of glycogen, and its protective action against oxidative stress. Together, these attributes can significantly improve aerobic endurance, cardiac function, and capacity as well as shorten recovery times (allowing higher intensity training), thereby enhancing performance. The purpose of this review is to highlight the most important mechanisms underlying the protective effect of meldonium against mitochondrial dysfunction (MD), which is responsible for oxidative stress, inflammation, and the cardiac changes known as \"athletic heart syndrome.\" Meldonium acts as an inhibitor of γ-butyrobetaine hydroxylase (BBOX), preventing the de novo synthesis of carnitine and its absorption at the intestinal level via the organic cation/carnitine transporter 2 (OCTN2) and directing the oxidation of fatty acids to the peroxisomes. The decrease in mitochondrial β-oxidation of fatty acids leads to a reduction in lipid peroxidation products that cause oxidative stress and prevent the formation of acyl/acetyl-carnitines involved in numerous pathological disorders. Given the recent findings of the potentially detrimental effects of prolonged high-intensity exercise on cardiovascular health and coronary atherosclerosis, there may be legitimate arguments for the justification of the use of substances like meldonium as protective supplements for athletes.