Inhibition of [3H]-LSD Binding to 5-HT7Receptors by Flavonoids fromScutellarialateriflora

Gafner, Stefan; Bergeron, Chantal; Batcha, Laura L; Reich, Jesse; Arnason, J. T.; Burdette, Joanna E.; Pezzuto, John M.; Angerhofer, Cindy K.

doi:10.1021/np0205102

Cited by 41 publications

(36 citation statements)

References 11 publications

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“…This compound is also found in Teucridium parvifolium, Tripora divaricata (Grayer et al, 2002), and Scutellaria lateriflora (Gafner et al, 2003). It has been reported that scutellarin was useful in the therapy of various ailments, such as cardiovascular diseases, sleep disorders, depression, migraine, pain, and memory impairment (Pouzet, 2002;Gafner et al, 2003;Goh et al, 2005). Today, it is commonly used in China as a remedy in dilating blood vessels, improving microcirculation, decreasing the viscosity of blood, reducing the blood platelet count, and inhibiting platelet aggregation activity (Hong and Liu, 2004;Liu et al, 2005).…”

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confidence: 80%

“…1), scutellarein 7-O-␤-D-glucuronide, is one of the major bioactive flavonoid glucuronides isolated from a Chinese herb, Erigeron breviscapus (Vant). This compound is also found in Teucridium parvifolium, Tripora divaricata (Grayer et al, 2002), and Scutellaria lateriflora (Gafner et al, 2003). It has been reported that scutellarin was useful in the therapy of various ailments, such as cardiovascular diseases, sleep disorders, depression, migraine, pain, and memory impairment (Pouzet, 2002;Gafner et al, 2003;Goh et al, 2005).…”

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confidence: 96%

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Pharmacokinetics and Metabolism of the Flavonoid Scutellarin in Humans After a Single Oral Administration

Chen¹,

Cui²,

Duan³

et al. 2006

Drug Metab Dispos

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ABSTRACT:Scutellarin is widely used in treating various cardiovascular diseases. Few data are available regarding its metabolism and pharmacokinetics in humans. The objectives of this study were to develop methods to identify major metabolites of scutellarin in human urine and plasma and to determine simultaneously the parent drug and its major metabolites in human plasma for pharmacokinetic studies. Four metabolites were detected in urine samples by liquid chromatography coupled with electrospray multistage mass spectrometry (MS), but only one of them was found in plasma. Its structure was confirmed as scutellarein 6-O-␤-D-glucuronide by MS, NMR, and UV absorbance spectra. The plasma concentrations of scutellarin and the major metabolite were simultaneously determined using liquid chromatography-tandem MS. After a single p.o. administration of 60 mg of scutellarin to 20 healthy subjects, the plasma concentrations of scutellarin were very low, and its plasma concentration-time curve was also anomalous. Plasma concentration of the major metabolite was comparatively high, and the peak plasma concentration was 87.0 ؎ 29.1 ng/ml. The T max was late (7.85 ؎ 1.62 h), and part of individual pharmacokinetic profiles showed double peaks, which indicated scutellarin could be absorbed into the intestine after hydrolysis to its aglycone by bacterial enzymes. This was followed by reconjugation in the intestinal cell and/or liver with glucuronic acid catalyzed by the phase II enzyme, which showed regioselectivity and species difference. The regioselectivity of glucuronoconjugation for scutellarin may be of importance for pharmacological activity. Plasma concentration of isoscutellarin can be used as a biomarker of scutellarin intake.

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confidence: 80%

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confidence: 96%

Pharmacokinetics and Metabolism of the Flavonoid Scutellarin in Humans After a Single Oral Administration

Chen¹,

Cui²,

Duan³

et al. 2006

Drug Metab Dispos

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“…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%

“…Gafner et al (2003) found extracts of dried S. lateriflora aerial parts and its flavonoids baicalin, scutellarin, wogonin, lateriflorein, ikonnikoside I and dihydrobaicalin, had high affinity for the serotonin 7 (5-HT 7 ) receptor in human 5-HT 7 -transfected Chinese hamster ovary cell lines. It was not known whether these extracts and flavonoids were agonists or antagonists (Gafner et al, 2003) but 5-HT 7 receptor antagonists and inverse agonists are known to be useful in the treatment of premenstrual syndrome, sleep disorders, appetite disorders, anxiety, phobias, panic, and stress-related disorders (Bright et al, 2004); these are also conditions for which S. lateriflora is traditionally used (Joshee et al, 2002;Greenfield and Davis, 2004).…”

Section: In Vitro Studiesmentioning

confidence: 99%

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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“…Ligands binding to the benzodiazepine site of the GABA A receptor decrease the likelihood of action potentials by excitatory neurotransmitters such as adrenalin and noradrenalin, implicated in anxiety and stress (Rabow et al 1995;Paladini et al 1999). Another study found both hot water and 70% ethanol extracts of whole aerial parts of S. lateriflora, as well as six major isolated flavonoids (baicalin, scutellarin, wogonin, lateriflorein, ikonnikoside I and dihydrobaicalin), bound to serotonin-7 (5-HT 7 ) receptors, suggesting the potential of S. lateriflora for attenuation of negative mood states (Gafner et al 2003).…”

Section: Introductionmentioning

confidence: 99%

The use of Scutellaria lateriflora: A pilot survey amongst herbal medicine practitioners

Brock

Whitehouse

Tewfik

et al. 2012

Journal of Herbal Medicine

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American skullcap (Scutellaria lateriflora) is a popular herb in traditional medicine systems and western Materia medica for anxiety and related disorders. It is reported to be one of the most widely used medicinal herbs, with anecdotal evidence for minimal side-effects and with no known toxicity. This article summarises the results of a pilot survey conducted amongst herbal medicine practitioners on their use of S. lateriflora.An email survey was conducted amongst herbal medicine practitioners in the UK and Ireland. It aimed to gather information on the extent of, and indications for, current use of S. lateriflora, its perceived effectiveness and its safety. Herbal medicine practitioners were selected from the membership list of the National Institute of Medical Herbalists (NIMH). All members with identifiable email addresses were contacted (n = 377) and responses were received from 62 (a 16% response rate).The results of the survey suggested that S. lateriflora is highly regarded among herbal medicine practitioners as an effective intervention for reducing anxiety and stress and is commonly prescribed for these conditions and related co-morbidities. The results were not conclusive as the response rate was low and respondents were only those with email access.

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Inhibition of [³H]-LSD Binding to 5-HT₇Receptors by Flavonoids fromScutellarialateriflora

Cited by 41 publications

References 11 publications

Pharmacokinetics and Metabolism of the Flavonoid Scutellarin in Humans After a Single Oral Administration

Pharmacokinetics and Metabolism of the Flavonoid Scutellarin in Humans After a Single Oral Administration

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

The use of Scutellaria lateriflora: A pilot survey amongst herbal medicine practitioners

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