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Plant Foods Hum Nutr. 2016 Dec;71(4):355-360.

Three-Step Test System for the Identification of Novel GABAA Receptor Modulating Food Plants.

Author information

1
Food Chemistry Unit, Department of Chemistry and Pharmacy, Emil Fischer Center, Friedrich-Alexander Universität Erlangen-Nürnberg (FAU), Schuhstr. 19, 91052, Erlangen, Germany.
2
Institute of Biochemistry, Emil Fischer Center, Friedrich-Alexander Universität Erlangen-Nürnberg (FAU), Fahrstr. 17, 91054, Erlangen, Germany.
3
Department of Biology, Friedrich-Alexander Universität Erlangen-Nürnberg (FAU), Staudtstr. 5, 91058, Erlangen, Germany.
4
Institute for Clinical Neurobiology, Universitätsklinikum Würzburg, Versbacherstr. 5, 97078, Würzburg, Germany.
5
Food Chemistry Unit, Department of Chemistry and Pharmacy, Emil Fischer Center, Friedrich-Alexander Universität Erlangen-Nürnberg (FAU), Schuhstr. 19, 91052, Erlangen, Germany. monika.pischetsrieder@fau.de.

Abstract

Potentiation of γ-amino butyric acid (GABA)-induced GABAA receptor (GABAAR) activation is a common pathway to achieve sedative, sleep-enhancing, anxiolytic, and antidepressant effects. Presently, a three-component test system was established for the identification of novel GABAAR modulating food plants. In the first step, potentiation of GABA-induced response of the GABAAR was analysed by two-electrode voltage clamp (TEVC) for activity on human α1β2-GABAAR expressed in Xenopus laevis oocytes. Positively tested food plants were then subjected to quantification of GABA content by high-performance liquid chromatography with fluorescence detection (HPLC-FLD) to exclude test foods, which evoke a TEVC-response by endogenous GABA. In the third step, specificity of GABAA-modulating activity was assessed by TEVC analysis of Xenopus laevis oocytes expressing the homologous glycine receptor (GlyR). The three-component test was then applied to screen 10 aqueous extracts of food plants for their GABAAR activity. Thus, hop cones (Humulus lupulus) and Sideritis sipylea were identified as the most potent specific GABAAR modulators eliciting significant potentiation of the current by 182 ± 27 and 172 ± 19 %, respectively, at the lowest concentration of 0.5 μg/mL. The extracts can now be further evaluated by in vivo studies and by structural evaluation of the active components.

KEYWORDS:

GABA; GABAA receptor; Glycine receptor; Hop cones; Lemon balm leaves; Sideritis

PMID:
27392961
DOI:
10.1007/s11130-016-0566-1
[Indexed for MEDLINE]

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