Tea catechins' affinity for human cannabinoid receptors

Korte, G. and Dreiseitel, A. and Schreier, P. and Oehme, A. and Locher, S. and Geiger, S. and Heilmann, J. and Sand, P. G. (2010) Tea catechins' affinity for human cannabinoid receptors. PHYTOMEDICINE, 17 (1). pp. 19-22. ISSN 0944-7113,

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Abstract

Among the many known health benefits of tea catechins count anti-inflammatory and neuroprotective activities, as well as effects on the regulation of food intake. Here we address cannabimimetic bioactivity of catechin derivatives occurring in tea leaves as a possible cellular effector of these functionalities. Competitive radioligand binding assays using recombinant human cannabinoid receptors expressed in Chem-1 and CHO cells identified (-)-epigallocatechin-3-O-gallate, EGCG (K(i)=33.6 mu M), (-)-epigallocatechin, EGC (K(i)=35.7 mu M), and (-)-epicatechin-3-O-gallate, ECC (K(i)=47.3 mu M) as ligands with moderate affinity for type I cannabinoid receptors, CBI. Binding to CB2 was weaker with inhibition constants exceeding 50 mu M for EGC and ECG. The epimers (+)-catechin and (-)epicatechin exhibited negligible affinities for both CB1 and CB2. It can be concluded that central nervous cannabinoid receptors may be targeted by selected tea catechins but signaling via peripheral type receptors is less likely to play a major role in vivo. (C) 2009 Elsevier GmbH. All rights reserved.

Item Type: Article
Uncontrolled Keywords: GREEN TEA; IN-VITRO; (-)-EPIGALLOCATECHIN GALLATE; EPIGALLOCATECHIN GALLATE; ENDOCANNABINOID SYSTEM; GABAERGIC SYSTEM; CONTROLLED-TRIAL; GALLOYL MOIETY; LIPID RAFTS; BLACK TEA; Camellia sinensis; Catechins; Epigallocatechin-3-O-gallate; Cannabinoid receptor; Neuroprotection
Subjects: 600 Technology > 610 Medical sciences Medicine
600 Technology > 615 Pharmacy
Divisions: Medicine > Lehrstuhl für Psychiatrie und Psychotherapie
Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann)
Depositing User: Dr. Gernot Deinzer
Date Deposited: 24 Aug 2020 08:23
Last Modified: 24 Aug 2020 08:23
URI: https://pred.uni-regensburg.de/id/eprint/25604

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