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- Publisher Website: 10.1016/S0006-2952(03)00233-8
- Scopus: eid_2-s2.0-0038005574
- PMID: 12818372
- WOS: WOS:000183820100013
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Article: 5,7-Dihydroxy-6-methoxyflavone, a benzodiazepine site ligand isolated from Scutellaria baicalensis Georgi, with selective antagonistic properties
Title | 5,7-Dihydroxy-6-methoxyflavone, a benzodiazepine site ligand isolated from Scutellaria baicalensis Georgi, with selective antagonistic properties |
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Authors | |
Keywords | Chemicals And Cas Registry Numbers |
Issue Date | 2003 |
Publisher | Elsevier 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? |
Abstract | As 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 Identifier | http://hdl.handle.net/10722/90850 |
ISSN | 2023 Impact Factor: 5.3 2023 SCImago Journal Rankings: 1.365 |
ISI Accession Number ID | |
References |
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Huen, MSY | en_HK |
dc.contributor.author | Leung, JWC | en_HK |
dc.contributor.author | Ng, W | en_HK |
dc.contributor.author | Lui, WS | en_HK |
dc.contributor.author | Chan, MNS | en_HK |
dc.contributor.author | Wong, JTF | en_HK |
dc.contributor.author | Xue, H | en_HK |
dc.date.accessioned | 2010-09-17T10:09:19Z | - |
dc.date.available | 2010-09-17T10:09:19Z | - |
dc.date.issued | 2003 | en_HK |
dc.identifier.citation | Biochemical Pharmacology, 2003, v. 66 n. 1, p. 125-132 | en_HK |
dc.identifier.issn | 0006-2952 | en_HK |
dc.identifier.uri | http://hdl.handle.net/10722/90850 | - |
dc.description.abstract | As 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.language | eng | en_HK |
dc.publisher | Elsevier Inc. The Journal's web site is located at http://www.elsevier.com/locate/biochempharm | en_HK |
dc.relation.ispartof | Biochemical Pharmacology | en_HK |
dc.subject | Chemicals And Cas Registry Numbers | en_HK |
dc.subject.mesh | Animals | en_HK |
dc.subject.mesh | Anti-Anxiety Agents - antagonists & inhibitors | en_HK |
dc.subject.mesh | Benzodiazepines - antagonists & inhibitors | en_HK |
dc.subject.mesh | Drugs, Chinese Herbal | en_HK |
dc.subject.mesh | Flavonoids - isolation & purification - pharmacology - therapeutic use | en_HK |
dc.subject.mesh | Ligands | en_HK |
dc.subject.mesh | Male | en_HK |
dc.subject.mesh | Maze Learning - drug effects | en_HK |
dc.subject.mesh | Mice | en_HK |
dc.subject.mesh | Mice, Inbred ICR | en_HK |
dc.subject.mesh | Motor Activity - drug effects | en_HK |
dc.subject.mesh | Picrotoxin | en_HK |
dc.subject.mesh | Plants, Medicinal - chemistry | en_HK |
dc.subject.mesh | Psychomotor Performance - drug effects | en_HK |
dc.subject.mesh | Radioligand Assay | en_HK |
dc.subject.mesh | Rats | en_HK |
dc.subject.mesh | Rats, Sprague-Dawley | en_HK |
dc.subject.mesh | Scutellaria baicalensis - chemistry | en_HK |
dc.subject.mesh | Seizures - chemically induced - prevention & control | en_HK |
dc.title | 5,7-Dihydroxy-6-methoxyflavone, a benzodiazepine site ligand isolated from Scutellaria baicalensis Georgi, with selective antagonistic properties | en_HK |
dc.type | Article | en_HK |
dc.identifier.email | Huen, MSY:huen.michael@hku.hk | en_HK |
dc.identifier.authority | Huen, MSY=rp01336 | en_HK |
dc.description.nature | link_to_subscribed_fulltext | - |
dc.identifier.doi | 10.1016/S0006-2952(03)00233-8 | en_HK |
dc.identifier.pmid | 12818372 | - |
dc.identifier.scopus | eid_2-s2.0-0038005574 | en_HK |
dc.relation.references | http://www.scopus.com/mlt/select.url?eid=2-s2.0-0038005574&selection=ref&src=s&origin=recordpage | en_HK |
dc.identifier.volume | 66 | en_HK |
dc.identifier.issue | 1 | en_HK |
dc.identifier.spage | 125 | en_HK |
dc.identifier.epage | 132 | en_HK |
dc.identifier.isi | WOS:000183820100013 | - |
dc.publisher.place | United States | en_HK |
dc.identifier.scopusauthorid | Huen, MSY=23004751500 | en_HK |
dc.identifier.scopusauthorid | Leung, JWC=35934996400 | en_HK |
dc.identifier.scopusauthorid | Ng, W=7401613396 | en_HK |
dc.identifier.scopusauthorid | Lui, WS=7101851160 | en_HK |
dc.identifier.scopusauthorid | Chan, MNS=36941304800 | en_HK |
dc.identifier.scopusauthorid | Wong, JTF=25939072200 | en_HK |
dc.identifier.scopusauthorid | Xue, H=37041779000 | en_HK |
dc.identifier.issnl | 0006-2952 | - |