Carvacrol modulates voltage-gated sodium channels kinetics in dorsal root ganglia

European Journal of Pharmacology
Humberto Cavalcante JocaJader Santos Cruz

Abstract

Recent studies have shown that many of plant-derived compounds interact with specific ion channels and thereby modulate many sensing mechanisms, such as nociception. The monoterpenoid carvacrol (5-isopropyl-2-methylphenol) has an anti-nociceptive effect related to a reduction in neuronal excitability and voltage-gated Na(+) channels (NaV) inhibition in peripheral neurons. However, the detailed mechanisms of carvacrol-induced inhibition of neuronal NaV remain elusive. This study explores the interaction between carvacrol and NaV in isolated dorsal root ganglia neurons. Carvacrol reduced the total voltage-gated Na(+) current and tetrodotoxin-resistant (TTX-R) Na(+) current component in a concentration-dependent manner. Carvacrol accelerates current inactivation and induced a negative-shift in voltage-dependence of steady-state fast inactivation in total and TTX-R Na(+) current. Furthermore, carvacrol slowed the recovery from inactivation. Carvacrol provoked a leftward shift in both the voltage-dependence of steady-state inactivation and activation of the TTX-R Na(+) current component. In addition, carvacrol-induced inhibition of TTX-R Na(+) current was enhanced by an increase in stimulation frequency and when neurons were pre-con...Continue Reading

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Citations

Sep 30, 2016·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Juliane C SilvaLucindo J Quintans-Júnior
Jan 21, 2017·Pharmaceutical Biology·Juan Carlos Ramos GonçalvesDemetrius Antônio Machado de Araújo
May 5, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ze-Jun Wang, Thomas Heinbockel
Jun 29, 2018·Acta Pharmacologica Sinica·Xiao-Yu ZhangYe-Hua Gan
Apr 28, 2020·BioMed Research International·Mantė AlmanaitytėRegina Mačianskienė
Dec 15, 2020·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Lícia T S PinaMairim R Serafini
Nov 5, 2019·Chemico-biological Interactions·Tiago Dos Santos-NascimentoJosé Henrique Leal-Cardoso

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