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

Beitrag in einer Fachzeitschrift


Details zur Publikation

Autor(en): Sahin S, Eulenburg V, Heinlein A, Villmann C, Pischetsrieder M
Zeitschrift: Journal of Functional Foods
Verlag: ELSEVIER SCIENCE BV
Jahr der Veröffentlichung: 2017
Band: 37
Seitenbereich: 641-649
ISSN: 1756-4646


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.



FAU-Autoren / FAU-Herausgeber

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


Autor(en) der externen Einrichtung(en)
Julius-Maximilians-Universität Würzburg


Zitierweisen

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://dx.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: 

Zuletzt aktualisiert 2018-29-06 um 11:23