Benzodiazepine Binding Site-Interactive Flavones from<i>Scutellaria baicalensis</i>Roots

Liao, Jyh‐Fei; Wang, Hui-Hung; Chen, Mingchih; Chen, Chien-Chih; Chen, Chieh-Fu

doi:10.1055/s-2006-957517

Cited by 33 publications

(23 citation statements)

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“…Affinity to the benzodiazepine site for scutellarein was moderate and weak for baicalin. Contrary to results of the earlier study (Liao et al, 1998) the binding affinities of wogonin and baicalein were strong. The authors suggested the discrepancy may be due to differences in species and assay models used (Hui et al, 2000).…”

Section: In Vitro Studiescontrasting

confidence: 99%

“…The receptor binding affinities of flavonoids present in S. lateriflora, including baicalein, baicalin, wogonin and scutellarein, to GABA A -BDZ receptor sites in vitro (Liao et al, 1998;Hui et al, 2000) indicates a possible anxiolytic action for the herb as does the presence of glutamine and the ability of certain S. lateriflora flavonoids to bind to 5HT 7 receptors in vitro (Gafner et al, 2003). The results of a survey amongst herbal medicine practitioners on their use of the herb and of a clinical study lend further support to its effectiveness as an anxiolytic.…”

Section: Summary and Evaluation Of Experimental Resultsmentioning

confidence: 99%

“…The Iroquai tribe, for example, used it 'to keep the throat clear' (Joshee et al, 2002). Conversely, S. baicalensis root is reported to have been used as a sedative (Liao et al, 1998).…”

Section: S Lateriflora Is the Practitioner's Choice For Treating Anxietymentioning

confidence: 99%

“…They bind to the benzodiazepine site of the GABA A receptor, thus increasing the affinity of the inhibitory neurotransmitter GABA for the GABA site of the GABA A receptor, decreasing the likelihood of action potentials by excitatory neurotransmitters (Rabow et al, 1995). A study (Liao et al, 1998), indicated oroxylin A, baicalein and wogonin, which are flavonoids found in S. lateriflora, had weak affinities for the benzodiazepine site of GABA A receptors in mouse cerebral cortex in vitro. In another study Hui et al (2000) tested the capacity of baicalin, baicalein, scutellarein and wogonin to bind to the benzodiazepine site of the GABA A receptor in homogenised rat brain.…”

Section: In Vitro Studiesmentioning

confidence: 99%

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American skullcap (Scutellaria lateriflora): an ancient remedy for today’s anxiety?

Brock

Whitehouse

Tewfik

et al. 2010

British Journal of Wellbeing

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Anxiety is a common but potentially serious disorder as it can lead to somatic and social dysfunction. Orthodox anxiolytics are associated with unpleasant side-effects and dependency. American skullcap (Scutellaria lateriflora) is a popular herb in traditional medicine systems and the western materia medica for anxiety and related disorders. Preliminary clinical and in vitro research provides encouraging support for its potential as a safe, well-tolerated and effective alternative. Key points• Research has demonstrated the capacity of American skullcap's flavonoids to bind to brain receptors implicated in modulation of anxiety • In one year up to one in six UK adults in the UK may suffer from an unexplained psychological disorder, the most common being anxiety • Anxiety and stress are common reasons for visits to herbal medicine practitioners.• An initial survey of UK and Ireland herbal medicine practitioners indicated American skullcap as their treatment of choice for anxiety and related disorders • Quality control of the raw herb and its commercial products is important.

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Section: In Vitro Studiescontrasting

confidence: 99%

Section: Summary and Evaluation Of Experimental Resultsmentioning

confidence: 99%

“…The Iroquai tribe, for example, used it 'to keep the throat clear' (Joshee et al, 2002). Conversely, S. baicalensis root is reported to have been used as a sedative (Liao et al, 1998).…”

Section: S Lateriflora Is the Practitioner's Choice For Treating Anxietymentioning

confidence: 99%

Section: In Vitro Studiesmentioning

confidence: 99%

See 2 more Smart Citations

American skullcap (Scutellaria lateriflora): an ancient remedy for today’s anxiety?

Brock

Whitehouse

Tewfik

et al. 2010

British Journal of Wellbeing

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“…Baicalein has been reported to have an affinity for the benzodiazepine binding site of GABA A receptors (23). Interestingly, the benzodiazepine receptors in peripheral tissues such as adrenals, kidney, and heart (2) enhance mitochondrial processing of human manganese-dependent SOD (Mn-SOD) precursor protein.…”

Section: Mechanism Of Baicalein Effect On Reperfusion Rosmentioning

confidence: 99%

Baicalein attenuates oxidant stress in cardiomyocytes

Shao

Hoek

Qin

et al. 2002

American Journal of Physiology-Heart and Circulatory Physiology

133

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Flavonoids within Scutellaria baicalensis may be potent antioxidants on the basis of our studies of S. baicalensis extract. To further this work, we studied the antioxidative effects of baicalein, a flavonoid component of S. baicalensis, in a chick cardiomyocyte model of reactive oxygen species (ROS) generation during hypoxia, simulated ischemia-reperfusion, or mitochondrial complex III inhibition with antimycin A. Oxidant stress was measured by oxidation of the intracellular probes 2Ј,7Ј-dichlorofluorescin diacetate and dihydroethidium. Viability was assessed by propidium iodide uptake. Baicalein attenuated oxidant stress during all conditions studied and acted within minutes of treatment. For example, baicalein given only at reperfusion dose dependently attenuated the ROS burst at 5 min after 1 h of simulated ischemia. It also decreased subsequent cell death at 3 h of reperfusion from 52.3 Ϯ 2.5% in untreated cells to 29.4 Ϯ 3.0% (with return of contractions; P Ͻ 0.001). In vitro studies using electron paramagnetic resonance spectroscopy with the spin trap 5-methoxycarbonyl-5-methyl-1-pyrroline-N-oxide revealed that baicalein scavenges superoxide but does not mimic the effects of superoxide dismutase. We conclude that baicalein can scavenge ROS generation in cardiomyocytes and that it protects against cell death in an ischemia-reperfusion model when given only at reperfusion.

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Herbal treatment following post‐seizure induction in rat by lithium pilocarpine: Scutellaria lateriﬂora (Skullcap), Gelsemium sempervirens (Gelsemium) and Datura stramonium (Jimson Weed) may prevent development of spontaneous seizures

Peredery

Persinger

2004

Phytotherapy Research

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About 1 week after the induction of status epilepticus in male rats by a single systemic injection of lithium (3 mEq/kg) and pilocarpine (30 g/kg), rats were continuously administered one of three herbal treatments through the water supply for 30 days. A fourth group received colloidal minerals and diluted food grade hydrogen peroxide in tap water, while a fifth group of rats received only tap water (control). Herbal treatments were selected for their historical antiseizure activities and sedative actions on the nervous system. The numbers of spontaneous seizures per day during a 15 min observation interval were recorded for each rat during the treatment period and during an additional 30 days when only tap water was given. Rats that received a weak solution of the three herbal fluid extracts of Scutellaria lateri flora (Skullcap), Gelsemium sempervirens (Gelsemium) and Datura stramonium (Jimson Weed) displayed no seizures during treatment while all the other groups were not seizure-free. However, when this treatment was removed, the rats in this group displayed numbers of spontaneous seizures comparable to the controls. Although there is no proof that herbal remedies can control limbic or temporal lobe epilepsy, the results of this experiment strongly suggest that the appropriate combination of herbal compounds may be helpful as adjunctive interventions.

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Benzodiazepine Binding Site-Interactive Flavones fromScutellaria baicalensisRoots

Cited by 33 publications

References 1 publication

American skullcap (Scutellaria lateriflora): an ancient remedy for today’s anxiety?

American skullcap (Scutellaria lateriflora): an ancient remedy for today’s anxiety?

Baicalein attenuates oxidant stress in cardiomyocytes

Herbal treatment following post‐seizure induction in rat by lithium pilocarpine: Scutellaria lateriﬂora (Skullcap), Gelsemium sempervirens (Gelsemium) and Datura stramonium (Jimson Weed) may prevent development of spontaneous seizures

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