Inhibition of Human Monoamine Oxidase: Biological and Molecular Modeling Studies on Selected Natural Flavonoids
Inhibition of Human Monoamine Oxidase: Biological and Molecular Modeling Studies on Selected Natural Flavonoids
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DOI：
10.1021/acs.jafc.6b03529
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发表时间：
2016-11-30
影响因子：
6.1
通讯作者：
Petzer, Jacobus P.
中科院分区：
文献类型：
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作者：
Carradori, Simone;Gidaro, Maria Concetta;Petzer, Jacobus P.
天然存在的类黄酮显示出过多的不同生物活性，但新出现的证据表明，这类化合物也可以作为抗抑郁剂，在中枢神经系统中具有多种作用机制，增加中枢神经传递，限制突触体对生物胺的重吸收，并调节神经内分泌和GABA（A）系统。由于它们存在于食品，食品衍生产品和营养保健品中，我们建立了它们作为可逆和竞争性人类单胺氧化酶（MAO）抑制剂的作用和结构-活性关系。此外，分子模拟研究，评估其模式的单胺氧化酶抑制，提出。这些发现可能为寻求新型药物样化合物和建立抗抑郁药物治疗中常见的有害药物-膳食补充剂相互作用提供关键影响。
Naturally occurring flavonoids display a plethora of different biological activities, but emerging evidence suggests that this class of compounds may also act as antidepressant agents endowed with multiple mechanisms of action in the central nervous system, increasing central neurotransmission, limiting the reabsorption of bioamines by synaptosomes, and modulating the neuroendocrine and GABA(A) systems. Due to their presence in foods, food-derived products, and nutraceuticals, we established their role and structure-activity relationships as reversible and competitive human monoamine oxidase (MAO) inhibitors. In addition, molecular modeling studies, which evaluated their modes of MAO inhibition, are presented. These findings could provide pivotal implications in the quest of novel drug-like compounds and for the establishment of harmful drug-dietary supplement interactions commonly reported in the therapy with antidepressant agents.