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DOI: 10.1055/s-0031-1298229
© Georg Thieme Verlag KG Stuttgart · New York
HPLC-based Activity Profiling – Discovery of Sanggenons as GABAA Receptor Modulators in the Traditional Chinese Drug Sang bai pi (Morus alba Root Bark)
Publication History
received October 10, 2011
revised Dec. 5, 2011
accepted Dec. 30, 2011
Publication Date:
31 January 2012 (online)
![](https://www.thieme-connect.de/media/plantamedica/201205/lookinside/thumbnails/10.1055-s-0031-1298229-1.jpg)
Abstract
EtOAc extracts from two batches of Morus alba root bark (Sang bai pi) potentiated γ-aminobutyric acid (GABA)-induced chloride influx in Xenopus oocytes, which transiently expressed GABAA receptors of the subunit composition α 1 β 2 γ 2S. With the aid of HPLC-based activity profiling of the extract from the first batch, activity was traced to a peak subsequently identified as sanggenon G (3). The second batch had a different phytochemical profile, and HPLC-based activity profiling led to the identification of sanggenon C (4) and a stereoisomer of sanggenon D (2) as positive GABAA receptor modulators. The structurally related compound kuwanon L (1) was inactive. The sanggenons represent a new scaffold of positive GABAA receptor modulators.
Key words
GABAA receptor modulator - Xenopus oocytes - HPLC-based activity profiling - sanggenon - Morus alba - Moraceae
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1 These authors contributed equally to this work.
Prof. Matthias Hamburger
Department of Pharmaceutical Sciences
University of Basel
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