Limonene has anti-anxiety activity via adenosine A2A receptor-mediated regulation of dopaminergic and GABAergic neuronal function in the striatum

Phytomedicine. 2021 Mar:83:153474. doi: 10.1016/j.phymed.2021.153474. Epub 2021 Jan 21.

Abstract

Background: Limonene, a common terpene found in citrus fruits, is assumed to reduce stress and mood disorders. Dopamine and γ-aminobutyric acid (GABA) have been reported to play an important role in modulating anxiety in different parts of the brain.

Hypothesis/purpose: Herein, we report the anxiolytic activity of limonene. In addition, we identified a possible mechanism underlying the effect of limonene on DAergic and GABAergic neurotransmission.

Study design: In this study, mice were injected with saline in the control group and limonene in the test group before behavioral analysis. We performed immunoblotting and high-performance liquid chromatography (HPLC) analysis after the behavioral study.

Results: The limonene treated group showed increased locomotor activity and open-arm preference in the elevated plus maze experiment. Limonene treatment increased the expression of both tyrosine hydroxylase and GAD-67 proteins and significantly upregulated dopamine levels in the striatum. Furthermore, tissue dopamine levels were increased in the striatum of mice following limonene treatment, and depolarization-induced GABA release was enhanced by limonene pre-treatment in PC-12 cells. Interestingly, limonene-induced anxiolytic activity and GABA release augmentation were blocked by an adenosine A2A receptor (A2AR) antagonist.

Conclusion: Our results suggest that limonene inhibits anxiety-related behavior through A2A receptor-mediated regulation of DAergic and GABAergic neuronal activity.

Keywords: Adenosine A2A receptor; Anxiety; Dopamine; GAD-67; Limonene; Tyrosine hydroxylase.

MeSH terms

  • Animals
  • Anti-Anxiety Agents / pharmacology*
  • Anxiety / drug therapy
  • Anxiety / metabolism
  • Behavior, Animal / drug effects
  • Corpus Striatum / drug effects*
  • Corpus Striatum / metabolism
  • Dopamine / metabolism
  • Dopaminergic Neurons / drug effects
  • Dopaminergic Neurons / metabolism
  • GABAergic Neurons / drug effects
  • GABAergic Neurons / metabolism
  • Limonene / pharmacology*
  • Locomotion / drug effects
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Rats
  • Receptor, Adenosine A2A / metabolism*
  • Synaptic Transmission / drug effects
  • Tyrosine 3-Monooxygenase / metabolism
  • gamma-Aminobutyric Acid / metabolism

Substances

  • Anti-Anxiety Agents
  • Receptor, Adenosine A2A
  • gamma-Aminobutyric Acid
  • Limonene
  • Tyrosine 3-Monooxygenase
  • Dopamine