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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
2013 Impact Factor: 4.650
2013 SCImago Journal Rankings: 1.994
 
DOIhttp://dx.doi.org/10.1016/S0006-2952(03)00233-8
 
ISI Accession Number IDWOS:000183820100013
 
ReferencesReferences in Scopus
 
DC FieldValue
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
2013 Impact Factor: 4.650
2013 SCImago Journal Rankings: 1.994
 
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
 
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Author Affiliations
  1. Hong Kong University of Science and Technology