Constituents of Sage (Salvia officinalis) with in vitro Affinity to Human Brain Benzodiazepine Receptor

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, ESI_pos-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

References

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