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

Hui, Kwok Min; Huen, Michael S.Y.; Wang, Hong Yan; Zheng, Hui; Sigel, Erwin; Baur, Roland; Ren, Huajian; Li, Zhi Wang; Wong, J. Tze‐Fei; Xue, Hong

doi:10.1016/s0006-2952(02)01347-3

Cited by 217 publications

(133 citation statements)

References 35 publications

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“…Since the discovery that certain flavonoids (namely flavones) specifically recognise the central BDZ receptors [7,8], efforts have been made to identify naturally occurring GABA A receptor benzodiazepine binding site ligands [5] to understand their interaction with these receptors [9][10][11][12] and to establish the CNS activity of different natural [13] and synthetic flavonoids [14,15]. Amongst these reports flavonoid derivatives with a flavone-like structure such as apigenin [16,17], chrysin [18] and wogonin [19] have been reported for their anxiolytic-like activity in different animal models of anxiety. These flavonoids with BDZ-receptor specificity and/or anxiolytic activity have been isolated from medicinal plants traditionally used in folk medicine for their anxiolytic/sedative properties such as Passiflora coerulea [20], Matricaria recutita [16], Tilia tomentosa [21], Jatropha cilliata [22], Salvia guaranitica [23], Matricaria chamomilla [17], Ziziphus jujuba [24].…”

Section: Introductionmentioning

confidence: 99%

Assessment of luteolin (3′,4′,5,7-tetrahydroxyflavone) neuropharmacological activity

Coleta

Campos

Cotrim

et al. 2008

Behavioural Brain Research

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Since the discovery that certain flavonoids (namely flavones) specifically recognise the central BDZ receptors, several efforts have been made to identify naturally occurring GABA A receptor benzodiazepine binding site ligands. Flavonoid derivatives with a flavone-like structure such as apigenin, chrysin and wogonin have been reported for their anxiolytic-like activity in different animal models of anxiety. Luteolin (3 ,4 ,5,7-tetrahydroxyflavone) is a widespread flavonoid aglycon that was reported as devoid of specific affinity for benzodiazepine receptor (BDZ-R) binding site, but its psychopharmacological activity is presently unknown. Considering (1) the close structural similarity with other active flavones, (2) the activity of some of its glycosilated derivatives and (3) the complexity of flavonoid effects in the central nervous system, luteolin was submitted to a battery of tests designed to evaluate its possible activity upon the CNS and its ability to interact with the BDZ-receptor binding sites was also analysed.Luteolin apparently has CNS activity with anxiolytic-like effects despite the low affinity for the BDZ-R shown in vitro. Our findings suggest a possible interaction with other neurotransmitter systems but we cannot rule out the possibility that luteolin's metabolites might show a higher affinity for the BDZ-R in vivo, thus eliciting the evident anxiolytic-like effects through a GABAergic mechanism.

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Section: Introductionmentioning

confidence: 99%

Assessment of luteolin (3′,4′,5,7-tetrahydroxyflavone) neuropharmacological activity

Coleta

Campos

Cotrim

et al. 2008

Behavioural Brain Research

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“…Quercetin, apigenin, morine, and chrysin have been shown to inhibit I GABA through α 1 β 1 γ 2s GABA A receptors [38]. Simple flavones appear to interact with the benzodiazepine binding site [34,39], whereas amentoflavone is a negative modulator of GABA A receptors whose action appears independent of benzodiazepine modulatory sites on the receptor [36]. Evidence for in vivo activity mediated through GABA A receptor modulation has been reported for selected flavonoids.…”

Section: Resultsmentioning

confidence: 99%

“…Evidence for in vivo activity mediated through GABA A receptor modulation has been reported for selected flavonoids. Simple flavones and flavonols such as chrysin, apigenin, wogonin, 6-methylapigenin, hispidulin, and luteolin-7-O-(2-rhamnosylglucoside) appear to induce predominantly anxiolytic effects and seem less efficient as sedatives, anticonvulsants, and myorelaxants [34,[39][40][41][42].…”

Section: Resultsmentioning

confidence: 99%

HPLC-based activity profiling for GABAA receptor modulators from the traditional Chinese herbal drug Kushen (Sophora flavescens root)

Yang¹,

Baburin²,

Plitzko³

et al. 2011

Mol Divers

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An EtOAc extract from the roots of Sophora flavescens (Kushen) potentiated γ -aminobutyric acid (GABA)-induced chloride influx in Xenopus oocytes transiently expressing GABA A receptors with subunit composition, α 1 β 2 γ 2S . HPLC-based activity profiling of the extract led to the identification of 8-lavandulyl flavonoids, kushenol I, sophoraflavanone G, (-)-kurarinone, and kuraridine as GABA A receptor modulators. In addition, a series of inactive structurally related flavonoids were characterized. Among these, kushenol Y (4) was identified as a new natural product. The 8-lavandulyl flavonoids are first representatives of a novel scaffold for the target.

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“…The major differences between the chemical structures are the presence and position of hydroxyl and methoxy groups. Previous studies involving baicalein and wogonin showed that these compounds influence multiple cellular processes (Shang et al, 2010;Wakabayashi & Yasui, 2000;Hui et al, 2002). In contrast, little is known about the activities of 6-hydroxyflavone and neobaicalein.…”

Section: Discussionmentioning

confidence: 99%

Wogonin and neobaicalein from Scutellaria litwinowii roots are apoptotic for HeLa cells

Tayarani-Najarani¹,

Asili²,

Parsaee³

et al. 2012

Rev. bras. farmacogn.

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Chemical investigation on the CH 2 Cl 2 fraction of the Scutellaria litwinowii Bornm. & Sint., Lamiaceace, root extract for the fi rst time resulted in the isolation of wogonin, and neobaicalein. These compounds were evaluated for their cytotoxicity towards HeLa cell lines and lymphocytes. Meanwhile, the role of apoptosis was explored in this toxicity. The cells were cultured in RPMI medium and incubated with different concentrations of isolated fl avonoids. Cell viability was quantifi ed by MTS assay. Apoptotic cells were determined using propidium iodide staining of DNA fragmentation by fl ow cytometry (sub-G1peak). Wogonin, and neobaicalein inhibited the growth of malignant cells in a dose-dependent manner. The IC50 values of 46.62 and 79.34 µM were, respectively, found for neobaicalein and wogonin against HeLa cells after 48 h of treatment. Neobaicalein induced a sub-G1 peak in the fl ow cytometry histogram of treated cells compared to control cells indicating that apoptotic cell death is involved in neobaicalein toxicity. Neobaicalein exerts cytotoxic and pro-apoptotic effects in HeLa cell lines and could be considered as a potential chemotherapeutic agent in cancer treatment.

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

Cited by 217 publications

References 35 publications

Assessment of luteolin (3′,4′,5,7-tetrahydroxyflavone) neuropharmacological activity

Assessment of luteolin (3′,4′,5,7-tetrahydroxyflavone) neuropharmacological activity

HPLC-based activity profiling for GABAA receptor modulators from the traditional Chinese herbal drug Kushen (Sophora flavescens root)

Wogonin and neobaicalein from Scutellaria litwinowii roots are apoptotic for HeLa cells

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