Abstract
A petroleum ether extract of the traditional Chinese herbal drug Duhuo (roots of Angelica pubescens Maxim. f. biserrata Shan et Yuan), showed significant activity in a functional two-microelectrode voltage clamp assay with Xenopus oocytes which expressed recombinant γ-aminobutyric acid type A (GABA A) receptors of the subtype α 1β 2γ 2S. HPLC-based activity profiling of the active extract revealed six compounds responsible for the GABA A receptor modulating activity. They were identified by microprobe NMR and high resolution mass spectrometry as columbianetin acetate ( 1), imperatorin ( 3), cnidilin ( 4), osthol ( 5), and columbianedin ( 6). In concentration-dependent experiments, osthol and cnidilin showed the highest potentiation of the GABA induced chloride current (273.6% ± 39.4% and 204.5% ± 33.2%, respectively at 300 μM). Bisabolangelone ( 2) only showed minor activity at the GABA A receptor. The example demonstrates that HPLC-based activity profiling is a simple and efficient method to rapidly identify GABA A receptor modulators in a bioactive plant extract.
Published Version
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