Taxodione, an abietane diterpenoid, was isolated from Salvia austriaca transformed roots grown in in vitro conditions. The compound is known to have antibacterial, cytotoxic and anti-tumour properties. This study evaluates the ability of pure taxodione and extracts obtained from the S. austriaca hairy roots and roots from field-grown plants to inhibit human acetylcholinesterase and butyrylcholinesterase. Both extracts were found to have similar actions against acetylcholinesterase. The IC50 for extracts from transformed and untransformed roots were 142.5 and 139.5 μg ml−1, respectively. The highest activity towards human acetylcholinesterase was demonstrated by taxodione (IC50 = 54.84 μg ml−1). With respect to BChE inhibition, the root extracts demonstrated stronger activity (IC50 = 23.6 μg ml−1: field-grown plants and 41.6 μg ml−1: transformed roots) than taxodione (IC50 = 195.9 μg ml−1). Taxodione showed significant cytotoxicity against A549 cell line (IC50 = 9.1 μg ml−1), whereas the activities for the extracts from S. austriaca roots of field-grown plants (IC50 = 75.7 μg ml−1) and hairy roots (IC50 = 86.2 μg ml−1) were lower. Computer modelling suggests that taxodione should not demonstrate cardiotoxic or genotoxic activity. It also indicates that taxodione should demonstrate very rapid transport from the body with very good blood–brain barrier penetration, but with no cumulative effect on the human body. The obtained results indicate that taxodione is a safe compound and may be used for further investigations in pharmacological activities. Copyright © 2015 John Wiley & Sons, Ltd.