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Inhibition of Human Monoamine Oxidase: Biological and Molecular Modeling Studies on Selected Natural Flavonoids

机译:人单胺氧化酶的抑制作用:天然黄酮类化合物的生物学和分子模型研究

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摘要

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.
机译:天然存在的类黄酮具有多种不同的生物活性,但新兴证据表明这类化合物还可以作为抗抑郁药,在中枢神经系统中具有多种作用机制,增加中枢神经传递,限制了突触小体对生物胺的再吸收,并调节神经内分泌和GABA(A)系统。由于它们在食品,食品衍生产品和保健食品中的存在,我们确立了它们作为可逆和竞争性人单胺氧化酶(MAO)抑制剂的作用和构效关系。此外,提出了分子模型研究,以评估其对MAO抑制的模式。这些发现可能对寻求新型药物样化合物以及建立抗抑郁药治疗中通常报道的有害药物-饮食补充相互作用具有关键意义。

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