Neurotoxic Effects of Linalool and β-Pinene on Tribolium castaneum Herbst

Molecules. 2017 Nov 24;22(12):2052. doi: 10.3390/molecules22122052.

Abstract

Effective, ethical pest control requires the use of chemicals that are highly specific, safe, and ecofriendly. Linalool and β-pinene occur naturally as major constituents of the essential oils of many plant species distributed throughout the world, and thus meet these requirements. These monoterpenes were tested as repellents against Tribolium castaneum, using the area preference method, after four hours of exposure and the effect transcriptional of genes associated with neurotransmission. Changes in gene expression of acetylcholinesterase (Ace1), GABA-gated anion channel splice variant 3a6a (Rdl), GABA-gated ion channel (Grd), glutamate-gated chloride channel (Glucl), and histamine-gated chloride channel 2 (Hiscl2) were assessed and the interaction with proteins important for the insect using in silico methods was also studied. For linalool and β-pinene, the repellent concentration 50 (RC50) values were 0.11 µL/cm² and 0.03 µL/cm², respectively. Both compounds induced overexpression of Hiscl2 gen in adult insects, and β-pinene also promoted the overexpression of Grd and the Ace1 gene. However, β-pinene and linalool had little potential to dock on computer-generated models for GABA-gated ion channel LCCH3, nicotinic acetylcholine receptor subunits alpha1 and alpha2, and putative octopamine/tyramine receptor proteins from T. castaneum as their respective binding affinities were marginal, and therefore the repellent action probably involved mechanisms other than direct interaction with these targets. Results indicated that β-pinene was more potent than linalool in inducing insect repellency, and also had a greater capacity to generate changes in the expression of genes involved in neuronal transmission.

Keywords: gene expression; insects; monoterpenes; repellents.

MeSH terms

  • Acetylcholinesterase / metabolism
  • Acyclic Monoterpenes
  • Animals
  • Bicyclic Monoterpenes
  • Bridged Bicyclo Compounds / pharmacology*
  • Gene Expression
  • Insect Control
  • Insect Repellents / pharmacology
  • Insecticides / pharmacology*
  • Molecular Docking Simulation
  • Monoterpenes / pharmacology*
  • Oils, Volatile / chemistry
  • Tribolium / drug effects*
  • Tribolium / genetics
  • Tribolium / metabolism

Substances

  • Acyclic Monoterpenes
  • Bicyclic Monoterpenes
  • Bridged Bicyclo Compounds
  • Insect Repellents
  • Insecticides
  • Monoterpenes
  • Oils, Volatile
  • beta-pinene
  • linalool
  • Acetylcholinesterase