Journal
MOLECULES
Volume 25, Issue 21, Pages -Publisher
MDPI
DOI: 10.3390/molecules25214873
Keywords
Monarda fistulosa; essential oils; calcium flux; TRPA1; monoterpene; carvacrol; thymol; β -myrcene
Funding
- National Institutes of Health IDeA Program [GM115371, GM103474]
- USDA National Institute of Food and Agriculture Hatch project [1009546]
- Montana State University Agricultural Experiment Station
- Tomsk Polytechnic University Competitiveness Enhancement Program [CEP-SAMT-208/2020]
- Program of Increasing the Competitiveness of TSU [8.2.10.2018]
Ask authors/readers for more resources
Little is known about the pharmacological activity of Monarda fistulosa L. essential oils. To address this issue, we isolated essential oils from the flowers and leaves of M. fistulosa and analyzed their chemical composition. We also analyzed the pharmacological effects of M. fistulosa essential oils on transient receptor potential (TRP) channel activity, as these channels are known targets of various essential oil constituents. Flower (MEOFl) and leaf (MEOLv) essential oils were comprised mainly of monoterpenes (43.1% and 21.1%) and oxygenated monoterpenes (54.8% and 77.7%), respectively, with a high abundance of monoterpene hydrocarbons, including p-cymene, gamma-terpinene, alpha-terpinene, and alpha-thujene. Major oxygenated monoterpenes of MEOFl and MEOLv included carvacrol and thymol. Both MEOFl and MEOLv stimulated a transient increase in intracellular free Ca2+ concentration ([Ca2+](i)) in TRPA1 but not in TRPV1 or TRPV4-transfected cells, with MEOLv being much more effective than MEOFl. Furthermore, the pure monoterpenes carvacrol, thymol, and beta-myrcene activated TRPA1 but not the TRPV1 or TRPV4 channels, suggesting that these compounds represented the TRPA1-activating components of M. fistulosa essential oils. The transient increase in [Ca2+](i) induced by MEOFl/MEOLv, carvacrol, beta-myrcene, and thymol in TRPA1-transfected cells was blocked by a selective TRPA1 antagonist, HC-030031. Although carvacrol and thymol have been reported previously to activate the TRPA1 channels, this is the first report to show that beta-myrcene is also a TRPA1 channel agonist. Finally, molecular modeling studies showed a substantial similarity between the docking poses of carvacrol, thymol, and beta-myrcene in the binding site of human TRPA1. Thus, our results provide a cellular and molecular basis to explain at least part of the therapeutic properties of these essential oils, laying the foundation for prospective pharmacological studies involving TRP ion channels.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available