Validation of the Target Protein of Insecticidal Dihydroagarofuran Sesquiterpene Polyesters.

Lina Lu,Qiuli Li,Wenjun Wu,Zhijun Qi

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.

Highlights

Identification of target proteins is the basis for development of new pesticides
Transmission electron microscopy (TEM) analysis showed that the midgut epithelial cells of Mythimna separata Walker larvae that ingested celangulin V (CV) were damaged, showing visible vacuolization of cytoplasm, serious disruption of microvilli, fragmentation of rough endoplasmic reticulum cisternae, and rupture of plasma membrane
Results showed that the subunit H of V-ATPase is the target proteinToxins of the dihydroagarofuran sesquiterpene polyesters

Summary

Introduction

Identification of target proteins is the basis for development of new pesticides. The discovery of novel targets may result in a series of new pesticides. From the root bark of Celastrus angulatus Max (Celastraceae) [4,5,6] These insecticidal compounds mainly affect the digestive system of pests, presenting a series of symptoms, such as excitement, twitching, emesis, and loss of body fluid after oral administration [7,8]. Transmission electron microscopy (TEM) analysis showed that the midgut epithelial cells of Mythimna separata Walker larvae that ingested celangulin V (CV) were damaged, showing visible vacuolization of cytoplasm, serious disruption of microvilli, fragmentation of rough endoplasmic reticulum cisternae, and rupture of plasma membrane These morphological changes induce leakage of cytoplasm contents into the midgut lumen, resulting in appearance of numerous lysosome-like vacuoles and secretion [8,9]

Methods

Results

Conclusion