File Download

There are no files associated with this item.

  Links for fulltext
     (May Require Subscription)
Supplementary

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

Title5,7-Dihydroxy-6-methoxyflavone, a benzodiazepine site ligand isolated from Scutellaria baicalensis Georgi, with selective antagonistic properties
Authors
KeywordsChemicals And Cas Registry Numbers
Issue Date2003
PublisherElsevier Inc. The Journal's web site is located at http://www.elsevier.com/locate/biochempharm
Citation
Biochemical Pharmacology, 2003, v. 66 n. 1, p. 125-132 How to Cite?
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.
Persistent Identifierhttp://hdl.handle.net/10722/90850
ISSN
2014 Impact Factor: 5.009
2014 SCImago Journal Rankings: 1.769
ISI Accession Number ID
References

 

DC FieldValueLanguage
dc.contributor.authorHuen, MSYen_HK
dc.contributor.authorLeung, JWCen_HK
dc.contributor.authorNg, Wen_HK
dc.contributor.authorLui, WSen_HK
dc.contributor.authorChan, MNSen_HK
dc.contributor.authorWong, JTFen_HK
dc.contributor.authorXue, Hen_HK
dc.date.accessioned2010-09-17T10:09:19Z-
dc.date.available2010-09-17T10:09:19Z-
dc.date.issued2003en_HK
dc.identifier.citationBiochemical Pharmacology, 2003, v. 66 n. 1, p. 125-132en_HK
dc.identifier.issn0006-2952en_HK
dc.identifier.urihttp://hdl.handle.net/10722/90850-
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.en_HK
dc.languageengen_HK
dc.publisherElsevier Inc. The Journal's web site is located at http://www.elsevier.com/locate/biochempharmen_HK
dc.relation.ispartofBiochemical Pharmacologyen_HK
dc.subjectChemicals And Cas Registry Numbersen_HK
dc.subject.meshAnimalsen_HK
dc.subject.meshAnti-Anxiety Agents - antagonists & inhibitorsen_HK
dc.subject.meshBenzodiazepines - antagonists & inhibitorsen_HK
dc.subject.meshDrugs, Chinese Herbalen_HK
dc.subject.meshFlavonoids - isolation & purification - pharmacology - therapeutic useen_HK
dc.subject.meshLigandsen_HK
dc.subject.meshMaleen_HK
dc.subject.meshMaze Learning - drug effectsen_HK
dc.subject.meshMiceen_HK
dc.subject.meshMice, Inbred ICRen_HK
dc.subject.meshMotor Activity - drug effectsen_HK
dc.subject.meshPicrotoxinen_HK
dc.subject.meshPlants, Medicinal - chemistryen_HK
dc.subject.meshPsychomotor Performance - drug effectsen_HK
dc.subject.meshRadioligand Assayen_HK
dc.subject.meshRatsen_HK
dc.subject.meshRats, Sprague-Dawleyen_HK
dc.subject.meshScutellaria baicalensis - chemistryen_HK
dc.subject.meshSeizures - chemically induced - prevention & controlen_HK
dc.title5,7-Dihydroxy-6-methoxyflavone, a benzodiazepine site ligand isolated from Scutellaria baicalensis Georgi, with selective antagonistic propertiesen_HK
dc.typeArticleen_HK
dc.identifier.emailHuen, MSY:huen.michael@hku.hken_HK
dc.identifier.authorityHuen, MSY=rp01336en_HK
dc.description.naturelink_to_subscribed_fulltext-
dc.identifier.doi10.1016/S0006-2952(03)00233-8en_HK
dc.identifier.pmid12818372en_HK
dc.identifier.scopuseid_2-s2.0-0038005574en_HK
dc.relation.referenceshttp://www.scopus.com/mlt/select.url?eid=2-s2.0-0038005574&selection=ref&src=s&origin=recordpageen_HK
dc.identifier.volume66en_HK
dc.identifier.issue1en_HK
dc.identifier.spage125en_HK
dc.identifier.epage132en_HK
dc.identifier.isiWOS:000183820100013-
dc.publisher.placeUnited Statesen_HK
dc.identifier.scopusauthoridHuen, MSY=23004751500en_HK
dc.identifier.scopusauthoridLeung, JWC=35934996400en_HK
dc.identifier.scopusauthoridNg, W=7401613396en_HK
dc.identifier.scopusauthoridLui, WS=7101851160en_HK
dc.identifier.scopusauthoridChan, MNS=36941304800en_HK
dc.identifier.scopusauthoridWong, JTF=25939072200en_HK
dc.identifier.scopusauthoridXue, H=37041779000en_HK

Export via OAI-PMH Interface in XML Formats


OR


Export to Other Non-XML Formats