Flavonoids are naturally occurring molecules present in the human diet. We
demonstrate that some flavonoids possess central nervous system effects act
ing through the central benzodiazepine receptors. The pharmacological chara
cterization of chrysin (5,7-dihydroxyflavone) and apigenin (5,7,4'-trihydro
xyflavone), isolated from Passiflora coerulea and Matricaria recutita, resp
ectively showed their anxiolytic, but not myorelaxant or amnesic effects. C
irsiliol (5,3',4'-trihydroxy-6,7-dimethoxyflavone), however isolated from S
alvia guaranitica, had sedative-depressant properties. We were able to incr
ease the biochemical and pharmacological potency of the natural flavonoids
by means of the addition of halo and/or nitro groups to the flavone nucleus
. Some flavonoids are partial agonists of the benzodiazepine receptors and
may become new therapeutic drugs, devoid of the unwanted side effects of cl
assical benzodiazepines.