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Rational Design of Photoactivatable Avermectin Derivatives Enabling Root-Mediated Translocation and Foliar

Jianyang Li1, Yanjun Zhang1, Xingyue Zhou1

  • 1Department of Applied Chemistry, China Agricultural University, Beijing 100193, China.

Journal of Agricultural and Food Chemistry
|May 19, 2026
PubMed
Summary

Novel avermectin derivatives with an o-nitrobenzyl group show enhanced plant mobility and sustained insecticidal activity. These photoactivatable compounds offer prolonged field efficacy, reducing application frequency and environmental risks.

Keywords:
DFTMD simulationsavermectino-nitrobenzylphotoactivatable

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Area of Science:

  • Agricultural Chemistry
  • Organic Chemistry
  • Plant Science

Background:

  • Avermectin's rapid UV degradation limits field efficacy to 3-5 days, necessitating frequent reapplication.
  • Frequent reapplication of avermectin increases costs and raises concerns regarding residues and ecological impact.
  • Current avermectin formulations face challenges in achieving sustained release and systemic translocation in plants.

Purpose of the Study:

  • To synthesize novel photoactivatable avermectin derivatives with enhanced systemic translocation and prolonged efficacy.
  • To investigate the potential of o-nitrobenzyl modification for improving compound mobility and preventing photodegradation.
  • To evaluate the insecticidal activity, plant transport, and photodegradation mechanisms of the new derivatives.

Main Methods:

  • Synthesis of avermectin derivatives via structural modification with an o-nitrobenzyl group.
  • Insecticidal activity assays to determine efficacy against target pests.
  • Plant transport and concentration profile studies to assess systemic translocation and persistence.
  • Computational chemistry to analyze photodegradation mechanisms and protein interactions.

Main Results:

  • Two highly active photoactivatable avermectin derivatives were successfully synthesized.
  • These derivatives demonstrated enhanced systemic mobility within plants compared to native avermectin.
  • Sustained concentration profiles and high insecticidal activity were observed, indicating prolonged efficacy.
  • Computational analysis elucidated the photodegradation pathway of the o-nitrobenzyl ester.

Conclusions:

  • The novel photoactivatable avermectin derivatives offer a promising solution for overcoming rapid UV degradation.
  • Enhanced systemic translocation and sustained release properties can significantly extend field efficacy.
  • These findings suggest a potential reduction in application frequency, leading to lower costs and reduced ecological risks.