Article first published online: 1 DEC 2015
DOI: 10.1002/ptr.5521
Copyright © 2015 John Wiley & Sons, Ltd.
Issue
Phytotherapy Research
- Abstract
- Article
- References
- Cited By
Keywords:
- cholinesterase inhibitors;
- Ellman method;
- diterpenoids;
- transformed roots
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.