Inhibition of human α7 nicotinic acetylcholine receptors by cyclic monoterpene carveol

Yosra Lozon, Ahmed Sultan, Stuart J. Lansdell, Tatiana Prytkova, Bassem Sadek, Keun Hang Susan Yang, Frank Christopher Howarth, Neil S. Millar, Murat Oz

Research output: Contribution to journalArticlepeer-review

19 Citations (Scopus)

Abstract

Cyclic monoterpenes are a group of phytochemicals with antinociceptive, local anesthetic, and anti-inflammatory actions. Effects of cyclic monoterpenes including vanilin, pulegone, eugenole, carvone, carvacrol, carveol, thymol, thymoquinone, menthone, and limonene were investigated on the functional properties of the cloned α7 subunit of the human nicotinic acetylcholine receptor expressed in Xenopus oocytes. Monoterpenes inhibited the α7 nicotinic acetylcholine receptor in the order carveol>thymoquinone>carvacrol>menthone>thymol>limonene>eugenole>pulegone≥carvone≥vanilin. Among the monoterpenes, carveol showed the highest potency on acetylcholine-induced responses, with IC50 of 8.3 μM. Carveol-induced inhibition was independent of the membrane potential and could not be reversed by increasing the concentration of acetylcholine. In line with functional experiments, docking studies indicated that cyclic monoterpenes such as carveol may interact with an allosteric site located in the α7 transmembrane domain. Our results indicate that cyclic monoterpenes inhibit the function of human α7 nicotinic acetylcholine receptors, with varying potencies.

Original languageEnglish
Pages (from-to)44-51
Number of pages8
JournalEuropean Journal of Pharmacology
Volume776
DOIs
Publication statusPublished - Apr 5 2016

Keywords

  • Carveol
  • Monoterpenes
  • Nicotinic acetylcholine receptor
  • Xenopus oocyte

ASJC Scopus subject areas

  • Pharmacology

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