Srinivasan V, Pandi-Perumal S R, Cardinali D P, Poeggeler B, Hardeland R
Department of Physiology, School of Medical Sciences, University Sains Malaysia, Kampus Kesihatan, 16150, Kubang kerian, Kelantan, Malaysia.
Behav Brain Funct. 2006 May 4;2:15. doi: 10.1186/1744-9081-2-15.
Increased oxidative stress and mitochondrial dysfunction have been identified as common pathophysiological phenomena associated with neurodegenerative disorders such as Alzheimer's disease (AD), Parkinson's disease (PD) and Huntington's disease (HD). As the age-related decline in the production of melatonin may contribute to increased levels of oxidative stress in the elderly, the role of this neuroprotective agent is attracting increasing attention. Melatonin has multiple actions as a regulator of antioxidant and prooxidant enzymes, radical scavenger and antagonist of mitochondrial radical formation. The ability of melatonin and its kynuramine metabolites to interact directly with the electron transport chain by increasing the electron flow and reducing electron leakage are unique features by which melatonin is able to increase the survival of neurons under enhanced oxidative stress. Moreover, antifibrillogenic actions have been demonstrated in vitro, also in the presence of profibrillogenic apoE4 or apoE3, and in vivo, in a transgenic mouse model. Amyloid-beta toxicity is antagonized by melatonin and one of its kynuramine metabolites. Cytoskeletal disorganization and protein hyperphosphorylation, as induced in several cell-line models, have been attenuated by melatonin, effects comprising stress kinase downregulation and extending to neurotrophin expression. Various experimental models of AD, PD and HD indicate the usefulness of melatonin in antagonizing disease progression and/or mitigating some of the symptoms. Melatonin secretion has been found to be altered in AD and PD. Attempts to compensate for age- and disease-dependent melatonin deficiency have shown that administration of this compound can improve sleep efficiency in AD and PD and, to some extent, cognitive function in AD patients. Exogenous melatonin has also been reported to alleviate behavioral symptoms such as sundowning. Taken together, these findings suggest that melatonin, its analogues and kynuric metabolites may have potential value in prevention and treatment of AD and other neurodegenerative disorders.
氧化应激增加和线粒体功能障碍已被确定为与神经退行性疾病相关的常见病理生理现象,如阿尔茨海默病(AD)、帕金森病(PD)和亨廷顿病(HD)。随着褪黑素分泌随年龄增长而减少可能导致老年人氧化应激水平升高,这种神经保护剂的作用正受到越来越多的关注。褪黑素作为抗氧化酶和促氧化酶的调节剂、自由基清除剂以及线粒体自由基形成的拮抗剂具有多种作用。褪黑素及其犬尿胺代谢产物通过增加电子流和减少电子泄漏直接与电子传递链相互作用的能力,是褪黑素能够在增强的氧化应激下提高神经元存活率的独特特性。此外,在体外,在存在促纤维化的载脂蛋白E4或载脂蛋白E3的情况下,以及在体内,在转基因小鼠模型中,均已证明其具有抗纤维化作用。褪黑素及其一种犬尿胺代谢产物可拮抗β淀粉样蛋白毒性。在几种细胞系模型中诱导的细胞骨架紊乱和蛋白质过度磷酸化已被褪黑素减弱,其作用包括应激激酶下调,并扩展到神经营养因子表达。AD、PD和HD的各种实验模型表明,褪黑素在拮抗疾病进展和/或减轻某些症状方面具有作用。已发现AD和PD患者的褪黑素分泌发生改变。试图弥补年龄和疾病相关的褪黑素缺乏的研究表明,给予这种化合物可以改善AD和PD患者的睡眠效率,并在一定程度上改善AD患者的认知功能。据报道,外源性褪黑素还可缓解诸如日落综合征等行为症状。综上所述,这些发现表明褪黑素及其类似物和犬尿代谢产物在预防和治疗AD及其他神经退行性疾病方面可能具有潜在价值。