Planta Med 2012; 78(3): 207-210
DOI: 10.1055/s-0031-1298171
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© Georg Thieme Verlag KG Stuttgart · New York

Discovery of GABAA Receptor Modulator Aristolactone in a Commercial Sample of the Chinese Herbal Drug “Chaihu” (Bupleurum chinense Roots) Unravels Adulteration by Nephrotoxic Aristolochia manshuriensis Roots

Diana C. Rueda1 , Janine Zaugg1 , Melanie Quitschau1 , Eike Reich2 , Steffen Hering3 , Matthias Hamburger1
  • 1Division of Pharmaceutical Biology, University of Basel, Basel, Switzerland
  • 2CAMAG Laboratory, Muttenz, Switzerland
  • 3Institute of Pharmacology and Toxicology, University of Vienna, Vienna, Austria
Further Information

Publication History

received August 24, 2011 revised Dec. 5, 2011

accepted Dec. 18, 2011

Publication Date:
23 January 2012 (online)

Abstract

In a two–microelectrode voltage clamp assay using Xenopus laevis oocytes, a petroleum ether extract prepared from a commercial sample of the traditional Chinese herbal drug labelled as “Chaihu” (Bupleurum chinense DC. roots) enhanced the I GABA by 156 % ± 22 % when tested at 100 µg/mL. By means of HPLC-based activity profiling combined with high-resolution LC-MS and microprobe NMR, the germacranolide aristolactone (1) was identified as one of the main active compounds (EC50 56.02 µM ± 5.09 µM). However, aristolactone has been previously reported only from the genus Aristolochia (Aristolochiaceae), suggesting a possible adulteration. With the aid of a validated HPTLC protocol for detection of aristolochic acids and with reference samples, the commercial sample was confirmed to be a mixture of Aristolochia manshuriensis root and Bupleurum chinense root. This finding was corroborated by macroscopic inspection of the drug. This case of adulteration with a highly nephrotoxic drug raises concerns about adequate quality control of TCM drugs commercialized in Europe.

Supporting Information

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Prof. Dr. Matthias Hamburger

Division of Pharmaceutical Biology
University of Basel

Klingelbergstrasse 50

4056 Basel

Switzerland

Phone: +41 6 12 67 14 25

Fax: +41 6 12 67 14 74

Email: Matthias.Hamburger@unibas.ch