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

Yang, Xinzhou ; Baburin, Igor ; Plitzko, Inken ; Hering, Steffen ; Hamburger, Matthias

In: Molecular Diversity, 2011, vol. 15, no. 2, p. 361-372

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    Titre
    • HPLC-based activity profiling for GABAA receptor modulators from the traditional Chinese herbal drug Kushen ( Sophora flavescens root)
    Auteur
    • Yang, Xinzhou. Institute of Pharmaceutical Biology, University of Basel, Klingelbergstrasse 50, 4056, Basel, Switzerland
    • Baburin, Igor. Institute of Pharmacology and Toxicology, University of Vienna, Althanstrasse 14, 1090, Vienna, Austria
    • Plitzko, Inken. Institute of Pharmaceutical Biology, University of Basel, Klingelbergstrasse 50, 4056, Basel, Switzerland
    • Hering, Steffen. Institute of Pharmacology and Toxicology, University of Vienna, Althanstrasse 14, 1090, Vienna, Austria
    • Hamburger, Matthias. Institute of Pharmaceutical Biology, University of Basel, Klingelbergstrasse 50, 4056, Basel, Switzerland
    Type de document
    • Postprint
    Identifiant OAI-PMH
    • oai:doc.rero.ch:313600
    Summary
    An EtOAc extract from the roots of Sophora flavescens (Kushen) potentiated γ-aminobutyric acid (GABA)-induced chloride influx in Xenopus oocytes transiently expressing GABAA 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 GABAA 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