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

• Published in: Journal of agricultural and food chemistry Vol. 64; no. 47; pp. 9004 - 9011
• Main Authors: Carradori, Simone, Gidaro, Maria Concetta, Petzer, Anél, Costa, Giosuè, Guglielmi, Paolo, Chimenti, Paola, Alcaro, Stefano, Petzer, Jacobus P
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 30.11.2016
• Subjects: Antidepressive Agents - pharmacology; Flavonoids - pharmacology; Humans; Inhibitory Concentration 50; Models, Molecular; Monoamine Oxidase - metabolism; Monoamine Oxidase Inhibitors - pharmacology; Structure-Activity Relationship; taxifolin; isorhamnetin; quercetin-3-O-glucoside; apigenin; naringin; monoamine oxidase inhibitor; eriocitrin; diosmetin; hesperidin
• ISSN: 0021-8561; 1520-5118
• DOI: 10.1021/acs.jafc.6b03529

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 GABAA 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.