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DOI: 10.1055/s-2003-37712
© Georg Thieme Verlag Stuttgart · New York
Constituents of Sage (Salvia officinalis) with in vitro Affinity to Human Brain Benzodiazepine Receptor
Prof. Dr. Dr. h.c. Waldemar Adam’s 65th birthdayPublication History
Received: June 24, 2002
Accepted: October 3, 2002
Publication Date:
07 March 2003 (online)
Abstract
Benzodiazepine receptor binding assay-guided fractionation of the methanol extract from sage leaves (Salvia officinalis L.) revealed three flavones and two abietane diterpenes functioning as benzodiazepine receptor-active components. Structural elucidation of the isolated pure compounds was performed by UV, EI-MS, ESIpos-MS/MS, as well as 1H- and 13C-NMR techniques. The flavones apigenin, hispidulin and cirsimaritin competitively inhibited 3 H-flumazenil binding to the benzodiazepine receptor with IC50 values of 30, 1.3 and 350 μM, respectively. In addition, the affinities of the newly discovered diterpene receptor ligands, i. e., 7-methoxyrosmanol and galdosol, were characterized. 7-Methoxyrosmanol exhibited an IC50 value of 7.2 μM and galdosol showed the strongest binding activity to the benzodiazepine receptor with an IC50 value of 0.8 μM.
Key words
Salvia officinalis L. - Lamiaceae - hispidulin - apigenin - cirsimaritin - 7-methoxyrosmanol - galdosol - benzodiazepine receptor
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Prof. Dr. P. Schreier
Institut für Pharmazie und Lebensmittelchemie
Universität Würzburg
Am Hubland
97074 Würzburg
Germany
Email: schreier@pzlc.uni-wuerzburg.de
Fax: +49-931-888-5484