title: Inhibition of Human Monoamine Oxidase: Biological and Molecular Modeling Studies on Selected Natural Flavonoids.
abstract: 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 GABAAsystems. 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.
authors.affiliation: Department of Pharmacy, "G. d'Annunzio" University of Chieti-Pescara , Via dei Vestini 31, 66100 Chieti, Italy.
authors.forename: Simone
authors.initials: S
authors.lastname: Carradori
authors.affiliation: Dipartimento di Scienze della Salute, "Magna Graecia" University of Catanzaro , Campus Universitario "S. Venuta", Viale Europa Loc. Germaneto, 88100 Catanzaro, Italy.
authors.forename: Maria Concetta
authors.initials: MC
authors.lastname: Gidaro
authors.affiliation: Centre of Excellence for Pharmaceutical Sciences, North-West University , Potchefstroom 2531, South Africa.
authors.forename: Anél
authors.initials: A
authors.lastname: Petzer
authors.affiliation: Dipartimento di Scienze della Salute, "Magna Graecia" University of Catanzaro , Campus Universitario "S. Venuta", Viale Europa Loc. Germaneto, 88100 Catanzaro, Italy.
authors.forename: Giosuè
authors.initials: G
authors.lastname: Costa
authors.affiliation: Department of Drug Chemistry and Technologies, Sapienza University of Rome , P.le A. Moro 5, 00185 Rome, Italy.
authors.forename: Paolo
authors.initials: P
authors.lastname: Guglielmi
authors.affiliation: Department of Drug Chemistry and Technologies, Sapienza University of Rome , P.le A. Moro 5, 00185 Rome, Italy.
authors.forename: Paola
authors.initials: P
authors.lastname: Chimenti
authors.affiliation: Dipartimento di Scienze della Salute, "Magna Graecia" University of Catanzaro , Campus Universitario "S. Venuta", Viale Europa Loc. Germaneto, 88100 Catanzaro, Italy.
authors.forename: Stefano
authors.initials: S
authors.lastname: Alcaro
authors.affiliation: Centre of Excellence for Pharmaceutical Sciences, North-West University , Potchefstroom 2531, South Africa.
authors.forename: Jacobus P
authors.initials: JP
authors.lastname: Petzer
mesh_terms: D000928:Antidepressive Agents / Q000494:pharmacology; D005419:Flavonoids / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D008995:Monoamine Oxidase / Q000378:metabolism*; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000928:Antidepressive Agents; D005419:Flavonoids; D008996:Monoamine Oxidase Inhibitors; D008995:Monoamine Oxidase
keywords: apigenin; diosmetin; eriocitrin; hesperidin; isorhamnetin; monoamine oxidase inhibitor; naringin; quercetin-3-O-glucoside; taxifolin