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Planta Med 2012; 78(5): 455-458
DOI: 10.1055/s-0031-1298174
Biological and Pharmacological Activity
Letters
© Georg Thieme Verlag KG Stuttgart · New York

GABAA Receptor Modulators from the Chinese Herbal Drug Junci Medulla – The Pith of Juncus effusus

Judith Singhuber1 , Igor Baburin2 , Sophia Khom2 , Martin Zehl1 , Ernst Urban3 , Steffen Hering2 , Brigitte Kopp1
  • 1Department of Pharmacognosy, University of Vienna, Vienna, Austria
  • 2Department of Pharmacology and Toxicology, University of Vienna, Vienna, Austria
  • 3Department of Medicinal Chemistry, University of Vienna, Vienna, Austria
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Publication History

received September 22, 2011 revised December 9, 2011

accepted December 18, 2011

Publication Date:
23 January 2012 (online)

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Abstract

The gamma-amino butyric acid (GABA) type A (GABAA) receptor represents a crucial target for clinical agents in the treatment of anxiety and insomnia. Using the two-microelectrode voltage clamp technique on recombinant α 1 β 2 γ 2S GABAA receptors, effusol (1) and dehydroeffusol (2) were isolated in a bioactivity-guided approach from the pith of Juncus effusus L. Both compounds concentration-dependently enhanced GABA induced chloride currents (IGABA) by a maximum 188 ± 20 (1) and 239 ± 18 % (2), independent of the benzodiazepine (BZ) binding site. This activity on the GABAA receptor may explain the traditional use of J. effusus as a sedative and anxiolytic agent in Chinese medicine.

Key words

Juncus effusus L. (Juncaceae) - GABA(A) receptor - voltage clamp - positive allosteric modulation - dehydroeffusol - effusol

Supporting Information

References

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Univ. Prof. Mag. Dr. Brigitte Kopp

Department of Pharmacognosy
University of Vienna

Althanstraße 14

1090 Vienna

Austria

Phone: +43 14 27 75 52 55

Fax: +43 14 27 75 52 56

Email: brigitte.kopp@univie.ac.at