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

  • Mol Divers. 2011 May;15(2):361-72. doi: 10.1007/s11030-010-9297-7.
Xinzhou Yang  1 ,  Igor Baburin ,  Inken Plitzko ,  Steffen Hering ,  Matthias Hamburger
Affiliations
  • 1. Institute of Pharmaceutical Biology, University of Basel, Klingelbergstrasse 50, 4056, Basel, Switzerland.
PMID: 21207144 DOI: 10.1007/s11030-010-9297-7
Abstract

An EtOAc extract from the roots of Sophora flavescens (Kushen) potentiated γ-aminobutyric acid (GABA)-induced chloride influx in Xenopus oocytes transiently expressing GABA(A) 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 GABA(A) 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.

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