Old pesticide, new use: Smart and safe enantiomer of isocarbophos in locust control

Locust plagues are still worldwide problems. Selecting active enantiomers from current chiral insecticides is necessary for controlling locusts and mitigating the pesticide pollution in agricultural lands. Herein, two enantiomers of isocarbophos (ICP) were separated and the enantioselectivity in insecticidal activity against the pest Locusta migratoria manilensis (L. migratoria) and mechanisms were investigated. The significant difference of LD50 between (+)-ICP (0.609 mg/kg bw) and (-)-ICP (79.412 mg/kg bw) demonstrated that (+)-ICP was a more effective enantiomer. The enantioselectivity in insecticidal activity of ICP enantiomers could be attributed to the selective affinity to acetylcholinesterase (AChE). Results of in vivo and in vitro assays suggested that AChE was more sensitive to (+)-ICP. In addition, molecular docking showed that the -CDOKER energies of (+)-ICP and (-)-ICP were 25.6652 and 24.4169, respectively, which suggested a stronger affinity between (+)-ICP and AChE. Significant selectivity also occurred in detoxifying enzymes activities (carboxylesterases (CarEs) and glutathione S-transferases (GSTs)) and related gene expressions. Suppression of detoxifying enzymes activities with (+)-ICP treatment suggested that (-)-ICP may induce the detoxifying enzyme-mediated ICP resistance. A more comprehensive understanding of the enantioselectivity of ICP is necessary for improving regulation and risk assessment of ICP.

Automated summary

Locust plagues remain a global issue, and selecting active enantiomers from chiral insecticides is crucial for controlling locusts. In this study, the enantioselectivity of two enantiomers of isocarbophos (ICP) against Locusta migratoria manilensis was investigated, with results showing that (+)-ICP had higher insecticidal activity attributed to its selective affinity to acetylcholinesterase. Additionally, significant selectivity was observed in detoxifying enzymes activities and related gene expressions, highlighting the importance of understanding the enantioselectivity of ICP for regulation and risk assessment purposes.