Chrysin (5,7-di-OH-flavone), a naturally-occurring ligand for benzodiazepine receptors, with anticonvulsant properties.
Chrysin (5,7-di-OH-flavone) was identified in Passiflora coerulea L., a plant used as a sedative in folkloric medicine. Chrysin was found to be a ligand for the benzodiazepine receptors, both central (Ki = 3 microM, competitive mechanism) and peripheral (Ki = 13 microM, mixed-type mechanism). Administered to mice by the intracerebroventricular route, chrysin was able to prevent the expression of tonic-clonic seizures induced by pentylenetertrazol. Ro 15-1788, a central benzodiazepine receptor antagonist, abolished this effect. In addition, all of the treated mice lose the normal righting reflex which suggests a myorelaxant action of the flavonoid. The presence in P. coerulea of benzodiazepine-like compounds was also confirmed.
Medina
J H
JH
Instituto de Biología Celular, Facultad de Medicina, Buenos Aires, Argentina.
Paladini
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Wolfman
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Levi de Stein
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Calvo
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Diaz
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Peña
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D000818:Animals; D000927:Anticonvulsants / Q000302:isolation & purification / Q000494:pharmacology*; D001667:Binding, Competitive; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology*; D005445:Flunitrazepam / Q000494:pharmacology; D013058:Mass Spectrometry; D051379:Mice; D010433:Pentylenetetrazole; D010936:Plant Extracts / Q000032:analysis*; D011869:Radioligand Assay; D011963:Receptors, GABA-A / Q000187:drug effects*; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control*
D000927:Anticonvulsants; D005419:Flavonoids; D010936:Plant Extracts; D011963:Receptors, GABA-A; C043561:chrysin; D005445:Flunitrazepam; D010433:Pentylenetetrazole