Modulation of T-type Ca2+ channels by Lavender and Rosemary extracts

PLoS One. 2017 Oct 26;12(10):e0186864. doi: 10.1371/journal.pone.0186864. eCollection 2017.

Abstract

Medicinal plants represent a significant reservoir of unexplored substances for early-stage drug discovery. Of interest, two flowering Mediterranean plants have been used for thousands of years for their beneficial effects on nervous disorders, including anxiety and mood. However, the therapeutic potential of these plants regarding their ability to target ion channels and neuronal excitability remains largely unknown. Towards this goal, we have investigated the ability of Lavender and Rosemary to modulate T-type calcium channels (TTCCs). TTCCs play important roles in neuronal excitability, neuroprotection, sensory processes and sleep. These channels are also involved in epilepsy and pain. Using the whole-cell patch-clamp technique, we have characterized how Lavender and Rosemary extracts, as well as their major active compounds Linalool and Rosmarinic acid, modulate the electrophysiological properties of recombinant TTCCs (CaV3.2) expressed in HEK-293T cells. Both the methanolic and essential oil extracts as well as the active compounds of these plants inhibit Cav3.2 current in a concentration-dependent manner. In addition, these products also induce a negative shift of the steady-state inactivation of CaV3.2 current with no change in the activation properties. Taken together, our findings reveal that TTCCs are a molecular target of the Lavender and Rosemary compounds, suggesting that inhibition of TTCCs could contribute to the anxiolytic and the neuroprotective effects of these plants.

MeSH terms

  • Animals
  • Calcium Channel Blockers / pharmacology
  • Calcium Channels, T-Type / drug effects*
  • Calcium Channels, T-Type / physiology
  • HEK293 Cells
  • Humans
  • Lavandula / chemistry*
  • Methanol / chemistry
  • Neurons / drug effects
  • Patch-Clamp Techniques
  • Plant Extracts / pharmacology*
  • Rosmarinus / chemistry*

Substances

  • Calcium Channel Blockers
  • Calcium Channels, T-Type
  • Plant Extracts
  • Methanol

Grants and funding

This work was supported by LabEx 'Ion Channel Science and Therapeutics' to PL. CEA was supported by ‘Bourse du Ministère de l’Enseignement Supérieur et de la Recherche Scientifique’ Maroc, Erasmus Mundus Averroes and L’Oréal-UNESCO for Women in Science Programs. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.