Expert Opin Investig Drugs. 2012 Nov;21(11):1593-6. doi: 10.1517/13543784.2012.716037. Epub 2012 Aug 23.
This editorial refers to "Cardiovascular effects of melatonin receptor agonists". The hormone melatonin is synthesized primarily in the pineal gland, retina, several peripheral tissues and organs. In the circulation, the concentration of melatonin follows a circadian rhythm, with high levels at night providing timing cues to target tissues endowed with melatonin receptors. Based on the data available, the last 18 years indicate that melatonin influences multiple factors of the cardiovascular function. Multiple evidences reveal that the rhythmicity of melatonin has a crucial role in a variety of cardiovascular pathophysiological processes including anti-inflammatory, antioxidant, anti-hypertensive and possibly as an antilipidemic function. Melatonin receptors receive and transduce melatonin's message to influence daily and seasonal rhythms of physiology. The melatonin message is translated through the interaction between the melatonin receptors (MT1 and MT2) and its coupling to G proteins, which are potential therapeutic targets in disorders ranging from insomnia, circadian sleep disorders, depression and cardiovascular diseases. Based on the data available, melatonin seems to have cardioprotective properties via its direct free radical scavenger activity. Melatonin efficiently interacts with several reactive oxygen species (receptor-independent actions). Collectively, these protective actions of melatonin may have potential clinical applicability for individuals with cardiovascular disease.
这篇社论提到了“褪黑素受体激动剂的心血管作用”。褪黑素主要在松果体、视网膜、几个外周组织和器官中合成。在循环中,褪黑素的浓度遵循昼夜节律,夜间水平高为具有褪黑素受体的靶组织提供时间线索。根据现有数据,过去 18 年表明褪黑素影响心血管功能的多种因素。多项证据表明,褪黑素的节律性在多种心血管病理生理过程中起着关键作用,包括抗炎、抗氧化、抗高血压,可能还有抗脂质功能。褪黑素受体接收并转导褪黑素的信息,以影响生理的日常和季节性节律。褪黑素的信息通过褪黑素受体(MT1 和 MT2)与其与 G 蛋白的相互作用来传递,这些 G 蛋白在从失眠、昼夜睡眠障碍、抑郁到心血管疾病等各种疾病中是潜在的治疗靶点。根据现有数据,褪黑素似乎通过其直接清除自由基的活性具有心脏保护特性。褪黑素有效地与几种活性氧物质(受体非依赖性作用)相互作用。总的来说,褪黑素的这些保护作用可能对患有心血管疾病的个体具有潜在的临床适用性。