Three-step test system for the identification of novel GABAa receptor modulating food plants

Journal article
(Original article)

Publication Details

Author(s): Sahin S, Eulenburg V, Kreis W, Villmann C, Pischetsrieder M
Journal: Plant Foods For Human Nutrition
Publisher: Springer Verlag (Germany)
Publication year: 2016
Volume: 71
Pages range: 355-360
ISSN: 0921-9668
Language: English


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.

FAU Authors / FAU Editors

Eulenburg, Volker PD Dr.
Lehrstuhl für Biochemie und Molekulare Medizin
Kreis, Wolfgang Prof. Dr.
Lehrstuhl für Pharmazeutische Biologie
Pischetsrieder, Monika Prof. Dr.
Lehrstuhl für Lebensmittelchemie (Henriette-Schmidt-Burkhardt Lehrstuhl)
Sahin, Sümeyye
Lehrstuhl für Lebensmittelchemie (Henriette-Schmidt-Burkhardt Lehrstuhl)

Additional Organisation
Emil-Fischer-Zentrum (Emil Fischer Center)

How to cite

Sahin, S., Eulenburg, V., Kreis, W., Villmann, C., & Pischetsrieder, M. (2016). Three-step test system for the identification of novel GABAa receptor modulating food plants. Plant Foods For Human Nutrition, 71, 355-360.

Sahin, Sümeyye, et al. "Three-step test system for the identification of novel GABAa receptor modulating food plants." Plant Foods For Human Nutrition 71 (2016): 355-360.


Last updated on 2018-19-04 at 03:32