| Modulation of GABAA receptors by valerian extracts is related to the content of valerenic acid. | |
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MedLine Citation:
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PMID: 18095218 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Valeriana Officinalis L . is a traditionally used sleep remedy, however, the mechanism of action and the substances responsible for its sedative and sleep-enhancing properties are not fully understood. As we previously identified valerenic acid as a subunit-specific allosteric modulator of GABAA receptors, we now investigated the relation between modulation of GABAA receptors by Valerian extracts of different polarity and the content of sesquiterpenic acids (valerenic acid, acetoxyvalerenic acid). All extracts were analysed by HPLC concerning the content of sesquiterpenic acids. GABAA receptors composed of alpha 1, beta 2 and gamma 2S subunits were expressed in Xenopus laevis oocytes and the modulation of chloride currents through GABAA receptors (IGABA) by Valerian extracts was investigated using the two-microelectrode voltage clamp technique. Apolar extracts induced a significant enhancement of IGABA, whereas polar extracts showed no effect. These results were confirmed by fractionating a highly active ethyl acetate extract: again fractions with high contents of valerenic acid exhibited strong receptor activation. In addition, removal of sesquiterpenic acids from the ethyl acetate extract led to a loss of I (GABA) enhancement. In conclusion, our data show that the extent of GABAA receptor modulation by Valerian extracts is related to the content of valerenic acid. |
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Authors:
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Gabriele Trauner; Sophia Khom; Igor Baburin; Birgit Benedek; Steffen Hering; Brigitte Kopp |
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Publication Detail:
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Type: Journal Article Date: 2007-12-19 |
Journal Detail:
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Title: Planta medica Volume: 74 ISSN: 0032-0943 ISO Abbreviation: Planta Med. Publication Date: 2008 Jan |
Date Detail:
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Created Date: 2008-01-25 Completed Date: 2008-04-15 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0066751 Medline TA: Planta Med Country: Germany |
Other Details:
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Languages: eng Pagination: 19-24 Citation Subset: IM |
Affiliation:
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Department of Pharmacognosy, University of Vienna, Vienna, Austria. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Chloride Channels / drug effects Female GABA Modulators / administration & dosage, pharmacology*, therapeutic use Indenes / chemistry Oocytes / drug effects, metabolism Patch-Clamp Techniques Phytotherapy* Plant Extracts / administration & dosage, chemistry, pharmacology*, therapeutic use Plant Roots Receptors, GABA-A / drug effects*, metabolism Sesquiterpenes / chemistry Valerian* Xenopus laevis |
| Chemical | |
Reg. No./Substance:
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0/Chloride Channels; 0/GABA Modulators; 0/Indenes; 0/Plant Extracts; 0/Receptors, GABA-A; 0/Sesquiterpenes; 3569-10-6/valerenic acid |
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