Abstract
Betonica officinalis (Lamiaceae) has been used in Austrian traditional medicine since ancient times against inflammatory disorders. The aim of this study was to investigate the anti-inflammatory properties of extracts, derived fractions, and isolated pure compounds of this plant by assessment of their effect on genes (E-selectin, IL-8) that are induced by inflammatory stimuli (TNF-α or LPS) in endothelial cells [1,2]. The plant material (herb) was extracted with dichloromethane (DCM) using an accelerated solvent extractor. Chlorophyll was separated by liquid-liquid-partition between DCM and a mixture of MeOH-H2O 1:1, in order to increase the concentration of the active compounds. Since the purified DCM extract showed strong activity in the mentioned assay, a bioactivity-guided fractionation was carried out. Subfractions were obtained by solid-phase extraction using C18 cartridges eluted with 30%, 70%, and 100% MeOH. The 30% and the 70% subfractions, which showed highest activity, were further fractionated by HPLC in order to identify and investigate their active constituents, whose structures were elucidated by HPLC-MS, 1D, and 2D NMR spectroscopy. Besides of some known polymethylated flavonoids (e.g. salvigenin), particularly the iridoid 8-O-acetylharpagide and two new diterpenoids were found to inhibit between 46% and 99% the LPS-stimulated induction of E-selectin at the concentration of 10µg/ml, evidencing a considerable potential as new anti-inflammatory agents. Acknowledgements: This work is funded by the Austrian Science Fund, NFN: S10704-B037.
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