Identification of eugenol as the major determinant of GABA(A)-receptor activation by aqueous Syzygium aromaticum L. (clove buds) extract

Sahin S, Eulenburg V, Heinlein A, Villmann C, Pischetsrieder M (2017)

Publication Status: Published

Publication Type: Journal article

Publication year: 2017

Journal

Journal of Functional Foods Elsevier

Publisher: ELSEVIER SCIENCE BV

Book Volume: 37

Pages Range: 641-649

DOI: 10.1016/j.jff.2017.08.033

Abstract

The spice Syzygium aromaticum L. (clove buds) exerts topical anesthetic and analgesic effects. Since GABA(A) receptors are an emerging drug target for pain treatment, the effects of aqueous clove extracts on the human alpha 1 beta 2-GABA(A) receptor were tested by two-electrode voltage clamp technique applying a three-step test system. The extract significantly and specifically potentiated the GABA-induced currents by an allosteric mechanism in concentration-dependent manner (0.5-5 mu g/mL up to 426 +/- 23%) HPLC-based activity-guided fractionation revealed eugenol as main determinant of this GABAergic activity. Acetyleugenol, an important component of clove bud oil, showed even higher activity than eugenol (1 mu g/mL; 308 +/- 26% versus 234 +/- 29%), but was detected in the aqueous extract only in trace amounts. Thus, the analgesic effects of clove might be partially mediated by positive modulation of the GABAA receptor and eugenol is a major contributor to this activity. (C) 2017 Elsevier Ltd. All rights reserved.

Authors with CRIS profile

Sümeyye Sahin Lehrstuhl für Lebensmittelchemie (Henriette-Schmidt-Burkhardt Lehrstuhl) Volker Eulenburg Lehrstuhl für Biochemie und Molekulare Medizin Anja Heinlein Lehrstuhl für Lebensmittelchemie (Henriette-Schmidt-Burkhardt Lehrstuhl) Monika Pischetsrieder Lehrstuhl für Lebensmittelchemie (Henriette-Schmidt-Burkhardt Lehrstuhl)

Involved external institutions

Julius-Maximilians-Universität Würzburg DE Germany (DE)

How to cite

APA:

Sahin, S., Eulenburg, V., Heinlein, A., Villmann, C., & Pischetsrieder, M. (2017). Identification of eugenol as the major determinant of GABA(A)-receptor activation by aqueous Syzygium aromaticum L. (clove buds) extract. Journal of Functional Foods, 37, 641-649. https://doi.org/10.1016/j.jff.2017.08.033

MLA:

Sahin, Sümeyye, et al. "Identification of eugenol as the major determinant of GABA(A)-receptor activation by aqueous Syzygium aromaticum L. (clove buds) extract." Journal of Functional Foods 37 (2017): 641-649.

BibTeX: Download