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Article: Anxiolytic effect of wogonin, a benzodiazepine receptor ligand isolated from Scutellaria baicalensis Georgi

TitleAnxiolytic effect of wogonin, a benzodiazepine receptor ligand isolated from Scutellaria baicalensis Georgi
Authors
KeywordsChemicals And Cas Registry Numbers
Issue Date2002
PublisherElsevier Inc. The Journal's web site is located at http://www.elsevier.com/locate/biochempharm
Citation
Biochemical Pharmacology, 2002, v. 64 n. 9, p. 1415-1424 How to Cite?
AbstractThe search for novel anxiolytics devoid of undesirable side-effects typical of classical benzodiazepines (BDZs) has been intense, and flavonoids, as a relative new class of ligands, have been shown to possess anxiolytic effects in vivo. The present study evaluated the pharmacological properties of a naturally occurring monoflavonoid, 5,7-dihydroxy-8-methoxyflavone or wogonin. The affinity (K i) of wogonin for the benzodiazepine site (BZD-S) on the γ-aminobutyric acid A (GABA A) receptor complex was 0.92 μM. Using electrophysiological techniques, we showed that wogonin enhanced the GABA-activated current in rat dorsal root ganglion neurons, and in Xenopus laevis oocytes expressing recombinant rat GABA A receptors, the enhancement was partially reversed by the co-application of a 1 μM concentration of the BZD-S antagonist anexate (Ro15-1788). Acute toxicity and behavioral effects were examined in mice. Acute lethal activity was low, with an LD 50 of 3.9 g/kg. Oral administration of wogonin (7.5 to 30 mg/kg) elicited an anxiolytic response that was similar to that elicited by diazepam in the elevated plus-maze; a dose-dependent increase in open arm entries and time spent in open arms was observed. More importantly, its anxiolytic effect was blocked by the co-administration of Ro15-1788. In the holeboard test, not only did wogonin-treated mice experience an increased number of head-dips but they also spent more time at it, showing no signs of sedation. Furthermore, wogonin did not cause myorelaxant effects in the horizontal wire test. Taken together, these data suggest that wogonin exerts its anxiolytic effect through positive allosteric modulation of the GABA A receptor complex via interaction at the BZD-S. Its anxiolytic effect was not accompanied by sedative and myorelaxant side-effects typical of BDZs. © 2002 Elsevier Science Inc. All rights reserved.
Persistent Identifierhttp://hdl.handle.net/10722/91142
ISSN
2015 Impact Factor: 5.091
2015 SCImago Journal Rankings: 2.263
ISI Accession Number ID
References

 

DC FieldValueLanguage
dc.contributor.authorHui, KMen_HK
dc.contributor.authorHuen, MSYen_HK
dc.contributor.authorWang, HYen_HK
dc.contributor.authorZheng, Hen_HK
dc.contributor.authorSigel, Een_HK
dc.contributor.authorBaur, Ren_HK
dc.contributor.authorRen, Hen_HK
dc.contributor.authorLi, ZWen_HK
dc.contributor.authorWong, JFen_HK
dc.contributor.authorXue, Hen_HK
dc.date.accessioned2010-09-17T10:13:40Z-
dc.date.available2010-09-17T10:13:40Z-
dc.date.issued2002en_HK
dc.identifier.citationBiochemical Pharmacology, 2002, v. 64 n. 9, p. 1415-1424en_HK
dc.identifier.issn0006-2952en_HK
dc.identifier.urihttp://hdl.handle.net/10722/91142-
dc.description.abstractThe search for novel anxiolytics devoid of undesirable side-effects typical of classical benzodiazepines (BDZs) has been intense, and flavonoids, as a relative new class of ligands, have been shown to possess anxiolytic effects in vivo. The present study evaluated the pharmacological properties of a naturally occurring monoflavonoid, 5,7-dihydroxy-8-methoxyflavone or wogonin. The affinity (K i) of wogonin for the benzodiazepine site (BZD-S) on the γ-aminobutyric acid A (GABA A) receptor complex was 0.92 μM. Using electrophysiological techniques, we showed that wogonin enhanced the GABA-activated current in rat dorsal root ganglion neurons, and in Xenopus laevis oocytes expressing recombinant rat GABA A receptors, the enhancement was partially reversed by the co-application of a 1 μM concentration of the BZD-S antagonist anexate (Ro15-1788). Acute toxicity and behavioral effects were examined in mice. Acute lethal activity was low, with an LD 50 of 3.9 g/kg. Oral administration of wogonin (7.5 to 30 mg/kg) elicited an anxiolytic response that was similar to that elicited by diazepam in the elevated plus-maze; a dose-dependent increase in open arm entries and time spent in open arms was observed. More importantly, its anxiolytic effect was blocked by the co-administration of Ro15-1788. In the holeboard test, not only did wogonin-treated mice experience an increased number of head-dips but they also spent more time at it, showing no signs of sedation. Furthermore, wogonin did not cause myorelaxant effects in the horizontal wire test. Taken together, these data suggest that wogonin exerts its anxiolytic effect through positive allosteric modulation of the GABA A receptor complex via interaction at the BZD-S. Its anxiolytic effect was not accompanied by sedative and myorelaxant side-effects typical of BDZs. © 2002 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 - isolation & purification - pharmacology - toxicityen_HK
dc.subject.meshBinding Sitesen_HK
dc.subject.meshDrugs, Chinese Herbal - pharmacologyen_HK
dc.subject.meshElectrophysiologyen_HK
dc.subject.meshFemaleen_HK
dc.subject.meshFlavanonesen_HK
dc.subject.meshFlavonoids - isolation & purification - pharmacology - toxicityen_HK
dc.subject.meshLigandsen_HK
dc.subject.meshMaleen_HK
dc.subject.meshMiceen_HK
dc.subject.meshMice, Inbred ICRen_HK
dc.subject.meshModels, Animalen_HK
dc.subject.meshMotor Activity - drug effectsen_HK
dc.subject.meshNeurons - drug effects - physiologyen_HK
dc.subject.meshPsychomotor Performance - drug effectsen_HK
dc.subject.meshRatsen_HK
dc.subject.meshRats, Sprague-Dawleyen_HK
dc.subject.meshReceptors, GABA-A - drug effects - metabolismen_HK
dc.subject.meshScutellaria baicalensis - chemistryen_HK
dc.subject.meshXenopus laevisen_HK
dc.titleAnxiolytic effect of wogonin, a benzodiazepine receptor ligand isolated from Scutellaria baicalensis Georgien_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(02)01347-3en_HK
dc.identifier.pmid12392823-
dc.identifier.scopuseid_2-s2.0-0036829634en_HK
dc.relation.referenceshttp://www.scopus.com/mlt/select.url?eid=2-s2.0-0036829634&selection=ref&src=s&origin=recordpageen_HK
dc.identifier.volume64en_HK
dc.identifier.issue9en_HK
dc.identifier.spage1415en_HK
dc.identifier.epage1424en_HK
dc.identifier.isiWOS:000178981800011-
dc.publisher.placeUnited Statesen_HK
dc.identifier.scopusauthoridHui, KM=7103304717en_HK
dc.identifier.scopusauthoridHuen, MSY=23004751500en_HK
dc.identifier.scopusauthoridWang, HY=36065838600en_HK
dc.identifier.scopusauthoridZheng, H=7403441193en_HK
dc.identifier.scopusauthoridSigel, E=7007154942en_HK
dc.identifier.scopusauthoridBaur, R=7103111366en_HK
dc.identifier.scopusauthoridRen, H=55041177900en_HK
dc.identifier.scopusauthoridLi, ZW=36063699100en_HK
dc.identifier.scopusauthoridWong, JF=25939072200en_HK
dc.identifier.scopusauthoridXue, H=37041779000en_HK

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