Chrysin (5,7-di-OH-flavone), a naturally-occurring ligand for benzodiazepine receptors, with anticonvulsant properties

Biochem Pharmacol. 1990 Nov 15;40(10):2227-31. doi: 10.1016/0006-2952(90)90716-x.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anticonvulsants / isolation & purification
  • Anticonvulsants / pharmacology*
  • Binding, Competitive
  • Flavonoids / isolation & purification
  • Flavonoids / pharmacology*
  • Flunitrazepam / pharmacology
  • Mass Spectrometry
  • Mice
  • Pentylenetetrazole
  • Plant Extracts / analysis*
  • Radioligand Assay
  • Receptors, GABA-A / drug effects*
  • Seizures / chemically induced
  • Seizures / prevention & control*

Substances

  • Anticonvulsants
  • Flavonoids
  • Plant Extracts
  • Receptors, GABA-A
  • chrysin
  • Flunitrazepam
  • Pentylenetetrazole