Zosima absinthifolia (ZA) extracts and the coumarins (+)-columbianadin and (-)-deltoin were evaluated for their potential hepatoprotective and antiinflamatory effects in a CCl(4)-induced hepatotoxicity assay in rats and by the inhibition of TNF-α production on LPS-stimulated THP-1 macrophages, respectively. Both the ZA extracts and the coumarins showed hepatoprotective activity confirmed by monitoring the ALT/AST levels and by histopathological examination. The antiinflamatory activity, proved by the inhibition of TNF-α production, was found to be higher for the n-hexane root extract than for coumarins, suggesting synergic potential of the extract. The concentration of (-)-deltoin and (+)-columbianadin in extracts was determined by HPLC analysis.