Validation of the Target Protein of Insecticidal Dihydroagarofuran Sesquiterpene Polyesters

Toxins (Basel). 2016 Mar 18;8(3):79. doi: 10.3390/toxins8030079.

Abstract

A series of insecticidal dihydroagarofuran sesquiterpene polyesters were isolated from the root bark of Chinese bittersweet (Celastrus angulatus Max). A previous study indicated that these compounds affect the digestive system of insects, and aminopeptidase N3 and V-ATPase have been identified as the most putative target proteins by affinity chromatography. In this study, the correlation between the affinity of the compounds to subunit H and the insecticidal activity or inhibitory effect on the activity of V-ATPase was analyzed to validate the target protein. Results indicated that the subunit H of V-ATPase was the target protein of the insecticidal compounds. In addition, the possible mechanism of action of the compounds was discussed. The results provide new ideas for developing pesticides acting on V-ATPase of insects.

Keywords: Mythimna separata Walker; V-ATPase; dihydroagarofuran sesquiterpene polyesters; subunit H of V-ATPase; target protein; target validation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CD13 Antigens / metabolism
  • Celastrus
  • Insect Proteins / antagonists & inhibitors
  • Insect Proteins / genetics
  • Insect Proteins / metabolism*
  • Insecticides / pharmacology*
  • Insecticides / toxicity
  • Larva / drug effects
  • Larva / enzymology
  • Lepidoptera / drug effects
  • Lepidoptera / enzymology
  • Lethal Dose 50
  • Plant Roots
  • Polyesters
  • Protein Subunits / antagonists & inhibitors
  • Protein Subunits / genetics
  • Protein Subunits / metabolism*
  • Recombinant Proteins / metabolism
  • Sesquiterpenes / pharmacology*
  • Sesquiterpenes / toxicity
  • Vacuolar Proton-Translocating ATPases / antagonists & inhibitors
  • Vacuolar Proton-Translocating ATPases / genetics
  • Vacuolar Proton-Translocating ATPases / metabolism*

Substances

  • Insect Proteins
  • Insecticides
  • Polyesters
  • Protein Subunits
  • Recombinant Proteins
  • Sesquiterpenes
  • dihydroagarofuran
  • CD13 Antigens
  • Vacuolar Proton-Translocating ATPases