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Friday, 6 July 2018

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. El Alaoui C1,2,3, Chemin J1,2, Fechtali T3, Lory P1,2. Author information 1 Institut de Génomique Fonctionnelle, CNRS, INSERM, University of Montpellier, Montpellier, France. 2 LabEx 'Ion Channel Science and Therapeutics', Montpellier, France. 3 Laboratoire de Neurosciences, Physiopathologies Intégrées et Substances Naturelles, Faculté des Sciences et Techniques Mohammedia, Université Hassan II, Casablanca, Morocco. 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. PMID: 29073181 PMCID: PMC5658086 DOI: 10.1371/journal.pone.0186864 [Indexed for MEDLINE] Free PMC Article