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Planta Med 2012; 78(5): 440-447
DOI: 10.1055/s-0031-1298229
Biological and Pharmacological Activity
Original Papers
© 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)

Hyun Jung Kim1 [*] , Igor Baburin2 [*] , Janine Zaugg1 , Samad Nejad Ebrahimi1 , 3 , Steffen Hering2 , Matthias Hamburger1
  • 1Department of Pharmaceutical Sciences, University of Basel, Basel, Switzerland
  • 2Institute of Pharmacology and Toxicology, University of Vienna, Vienna, Austria
  • 3Department of Phytochemistry, Medicinal Plant and Drugs Research Institute, Shahid Beheshti University, G. C., Tehran, Iran
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Publikationsverlauf

received October 10, 2011 revised Dec. 5, 2011

accepted Dec. 30, 2011

Publikationsdatum:
31. Januar 2012 (online)

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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

Supporting Information

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1 These authors contributed equally to this work.

Prof. Matthias Hamburger

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University of Basel

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