Article: 5,7-Dihydroxy-6-methoxyflavone, a benzodiazepine site ligand isolated from Scutellaria baicalensis Georgi, with selective antagonistic properties

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Title5,7-Dihydroxy-6-methoxyflavone, a benzodiazepine site ligand isolated from Scutellaria baicalensis Georgi, with selective antagonistic properties
AuthorsHuen, MSY1
Leung, JWC1
Ng, W1
Lui, WS1
Chan, MNS1
Wong, JTF1
Xue, H1
KeywordsChemicals And Cas Registry Numbers
Issue Date2003
PublisherElsevier Inc. The Journal's web site is located at http://www.elsevier.com/locate/biochempharm
CitationBiochemical Pharmacology, 2003, v. 66 n. 1, p. 125-132 [How to Cite?]
DOI: http://dx.doi.org/10.1016/S0006-2952(03)00233-8
AbstractAs part of an effort to identify naturally occurring GABA A receptor benzodiazepine binding site (BDS) ligands from traditional medicinal herbs, we previously reported that flavonoid derivatives isolated from Scutellaria baicalensis (S. baicalensis) Georgi exhibited significant affinities for the BDS. The present study describes the characterization of 5,7-dihydroxy-6-methoxyflavone (oroxylin A), one of the major components of the herbal extract. Oroxylin A inhibited [ 3H]flunitrazepam binding to rat cerebral cortical membrane with a IC 50 value of 1.09±0.07μM. A GABA ratio of 1.09±0.04 suggests that oroxylin A interacts as an antagonist at the recognition site. In neuropharmacological studies, oral administration of oroxylin A (3.75-60mgkg -1) did not result in significant changes in animal models routinely employed for benzodiazepine (BD) evaluation. However, oroxylin A selectively abolished the anxiolytic, myorelaxant and motor incoordination, but not the sedative and anticonvulsant effects elicited by diazepam, a BDS agonist. These results add oroxylin A to the list of CNS active flavonoids, and as the first naturally occurring member endowed with selective antagonistic actions via the BDS. © 2003 Elsevier Science Inc. All rights reserved.
ISSN0006-2952
2011 Impact Factor: 4.705
2011 SCImago Journal Rankings: 0.418
DOIhttp://dx.doi.org/10.1016/S0006-2952(03)00233-8
ReferencesReferences in Scopus
DC Field
Value
dc.contributor.authorHuen, MSY
dc.contributor.authorLeung, JWC
dc.contributor.authorNg, W
dc.contributor.authorLui, WS
dc.contributor.authorChan, MNS
dc.contributor.authorWong, JTF
dc.contributor.authorXue, H
dc.date.accessioned2010-09-17T10:09:19Z
dc.date.available2010-09-17T10:09:19Z
dc.date.issued2003
dc.description.abstractAs part of an effort to identify naturally occurring GABA A receptor benzodiazepine binding site (BDS) ligands from traditional medicinal herbs, we previously reported that flavonoid derivatives isolated from Scutellaria baicalensis (S. baicalensis) Georgi exhibited significant affinities for the BDS. The present study describes the characterization of 5,7-dihydroxy-6-methoxyflavone (oroxylin A), one of the major components of the herbal extract. Oroxylin A inhibited [ 3H]flunitrazepam binding to rat cerebral cortical membrane with a IC 50 value of 1.09±0.07μM. A GABA ratio of 1.09±0.04 suggests that oroxylin A interacts as an antagonist at the recognition site. In neuropharmacological studies, oral administration of oroxylin A (3.75-60mgkg -1) did not result in significant changes in animal models routinely employed for benzodiazepine (BD) evaluation. However, oroxylin A selectively abolished the anxiolytic, myorelaxant and motor incoordination, but not the sedative and anticonvulsant effects elicited by diazepam, a BDS agonist. These results add oroxylin A to the list of CNS active flavonoids, and as the first naturally occurring member endowed with selective antagonistic actions via the BDS. © 2003 Elsevier Science Inc. All rights reserved.
dc.description.natureLink_to_subscribed_fulltext
dc.identifier.citationBiochemical Pharmacology, 2003, v. 66 n. 1, p. 125-132 [How to Cite?]
DOI: http://dx.doi.org/10.1016/S0006-2952(03)00233-8
dc.identifier.doihttp://dx.doi.org/10.1016/S0006-2952(03)00233-8
dc.identifier.epage132
dc.identifier.isiWOS:000183820100013
dc.identifier.issn0006-2952
2011 Impact Factor: 4.705
2011 SCImago Journal Rankings: 0.418
dc.identifier.issue1
dc.identifier.pmid12818372
dc.identifier.scopuseid_2-s2.0-0038005574
dc.identifier.spage125
dc.identifier.urihttp://hdl.handle.net/10722/90850
dc.identifier.volume66
dc.languageeng
dc.publisherElsevier Inc. The Journal's web site is located at http://www.elsevier.com/locate/biochempharm
dc.publisher.placeUnited States
dc.relation.ispartofBiochemical Pharmacology
dc.relation.referencesReferences in Scopus
dc.subject.meshAnimals
dc.subject.meshAnti-Anxiety Agents - antagonists & inhibitors
dc.subject.meshBenzodiazepines - antagonists & inhibitors
dc.subject.meshDrugs, Chinese Herbal
dc.subject.meshFlavonoids - isolation & purification - pharmacology - therapeutic use
dc.subject.meshLigands
dc.subject.meshMale
dc.subject.meshMaze Learning - drug effects
dc.subject.meshMice
dc.subject.meshMice, Inbred ICR
dc.subject.meshMotor Activity - drug effects
dc.subject.meshPicrotoxin
dc.subject.meshPlants, Medicinal - chemistry
dc.subject.meshPsychomotor Performance - drug effects
dc.subject.meshRadioligand Assay
dc.subject.meshRats
dc.subject.meshRats, Sprague-Dawley
dc.subject.meshScutellaria baicalensis - chemistry
dc.subject.meshSeizures - chemically induced - prevention & control
dc.subjectChemicals And Cas Registry Numbers
dc.title5,7-Dihydroxy-6-methoxyflavone, a benzodiazepine site ligand isolated from Scutellaria baicalensis Georgi, with selective antagonistic properties
dc.typeArticle
Author Affiliations
  1. Hong Kong University of Science and Technology