The discovery of transient receptor potential (TRP) ion channels in cardiac muscle has made them a promising target for the treatment of heart failure due to their activation markedly increasing cardiac contractility. Essential oils isolated from the plant Ferula iliensis (FiEOs) have great potential to be potent TRP agonists based on their structural homology to capsaicin (CAP) and allyl isothiocyanate (AITC), TRP vanilloid1 (TRPV1) and TRP ankyrin1 (TRPA1) agonists, respectively. HEK293 cells expressing TRPV1 or TRPA1 were used to assess the extent to which FiEOs were capable of activating TRPV1 or TRPA1 ion channels. Intracellular free Ca2+ concentration ([Ca2+]i) was measured to determine the magnitude of the response. (-)-Linalool, (-)-Limonene, and Camphene elicited transient increases in [Ca2+]i similar to those observed with CAP in TRPV1-transfected HEK293 cells while α-Pinene oxide and α-Terpineol elicited transient increases in [Ca2+]i similar to those observed with AITC in TRPA1-transfected HEK293 cells. No transient increases in [Ca2+]i were observed by any of the FiEOs in non-transfected HEK293 cells, indicating the responses were specifically mediated by activation of TRPV1 or TRPA1 ion channels. Novel plant-based FiEOs that elicit TRPV1 and TRPA1 responses could potentially be viable and attractive products in the multi-billion-dollar alternative medicine industry for the treatment of a variety of types of heart failure. Further studies of FiEOs could lead to the development of natural therapeutic strategies for increased cardiac output via TRPV1 and TRPA1 stimulation.
Dr. Derek Damron
Ms. Monica Ghosh
Activation of transient receptor potential (TRP) ion channels has been shown to markedly increase cardiac contractility, making them promising targets for heart failure treatment. Essential oils isolated from the plant Ferula iliensis (FiEOs) have similar chemical structures to TRP vanilloid1 (TRPV1) and TRP ankyrin1 (TRPA1) agonists, leading us to hypothesize that FiEOs could be potent TRP agonists. HEK293 cells expressing TRPV1 or TRPA1 were used to assess the extent to which 30 different FiEOs could elicit transient intracellular free Ca2+ ([Ca2+]) increases. Several FiEOs elicited transient [Ca2+] increases in TRPV1- and TRPA1- transfected HEK293 cells. No transients were observed in non-transfected HEK293 cells, suggesting the responses were TRP-mediated. Further studies of FiEOs could lead to natural treatments for various types heart failure.
Hopkins, E., Ghosh, M., & Damron, D. (2018). Essential Oils Isolated from Ferula iliensis Modulate Transient Receptor Potential Ion Channels. https://oaks.kent.edu/node/5710
Hopkins, Erik, Monica Ghosh, and Derek Damron. 2018. “Essential Oils Isolated from Ferula Iliensis Modulate Transient Receptor Potential Ion Channels”. https://oaks.kent.edu/node/5710.
Hopkins, E., M. Ghosh, and D. Damron. Essential Oils Isolated from Ferula Iliensis Modulate Transient Receptor Potential Ion Channels. 5 Apr. 2018, https://oaks.kent.edu/node/5710.