Flavonoids and the Central Nervous System: from Forgotten Factors to Potent Anxiolytic Compounds

Authors: Paladini A.C.1; Marder M.1; Viola H.1; Wolfman C.1; Wasowski C.1; Medina J.H.1

Source: Journal of Pharmacy and Pharmacology, Volume 51, Number 5, 1 May 1999 , pp. 519-526(8)

Publisher: Pharmaceutical Press

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Abstract:

The list of activities of plant flavonoids did not include effects on the central nervous system (CNS) up to 1990, when our laboratory described the existence of natural anxiolytic flavonoids. The first of these was chrysin (5,7-dihydroxyflavone), followed by apigenin (5,7,4prime-trihydroxyflavone) and flavone itself. Semisynthetic derivatives of flavone obtained by introducing halogens, nitro groups or both in its molecule, give rise to high affinity ligands for the benzodiazepine receptor, active in-vivo; 6,3prime-dinitroflavone, for example, is an anxiolytic drug 30 times more potent than diazepam.

The data collected in this paper make clear that some natural flavonoids are CNS-active molecules and that the chemical modification of the flavone nucleus dramatically increases their anxiolytic potency.

Document Type: Research article

DOI: 10.1211/0022357991772790

Affiliations: 1: Instituto de Quimica y Fisicoquimica Biologicas Instituto de Biologia Celular, Facultad de Farmacia y Bioquimica, Junin 956 (1113) Facultad de Medicina, Paraguay 2155, Buenos Aires (1121) Buenos Aires, Argentina Argentina

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