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农药选择性的分子机制:来自杀螨剂毒理学的见解。

Molecular mechanisms of pesticide selectivity: Insights from acaricide toxicology.

作者信息

İnak Emre, De Rouck Sander, Van Leeuwen Thomas

机构信息

Department of Plant Protection, Faculty of Agriculture, Ankara University, Dıskapı, 06110 Ankara, Türkiye.

Laboratory of Agrozoology, Department of Plants and Crops, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, 9000 Ghent, Belgium.

出版信息

Pestic Biochem Physiol. 2025 Sep;213:106537. doi: 10.1016/j.pestbp.2025.106537. Epub 2025 Jul 1.

Abstract

Broad-spectrum pesticides have been used for decades to control a wide range of crop pests and vectors of human and animal diseases. However, concerns about the environment and human health have provided a strong impetus to design more selective molecules that can be safely used in integrated pest management (IPM) programs. In addition, selectivity is crucial for the direct use of compounds on humans and animals, with in-hive use of acaricides for treatment of Varroa on bees as an extreme example. Pesticide selectivity is mainly achieved via physiological or ecological factors. The mechanisms underlying physiological selectivity can be based on either differential penetration, excretion or metabolism, differences in affinity of the target-site proteins, or a combination of both. Metabolism-based selectivity can be achieved both through species-specific activation, as well as detoxification. Many acaricides, compounds that specifically target mite and tick species, are highly selective with little efficacy on insects. This selectivity has been documented for historical reference acaricides that have been used for several decades, but also for more recently developed chemicals. Molecular insights into the mechanisms of selectivity are crucial in devising new compounds that specifically target certain pests. In this review, we provide an overview of what is known about the molecular mechanisms of acaricide selectivity.

摘要

广谱杀虫剂已被使用数十年,用于控制各种农作物害虫以及人类和动物疾病的病媒。然而,对环境和人类健康的担忧有力地推动了人们设计更具选择性的分子,以便能够安全地用于综合虫害管理(IPM)计划。此外,选择性对于化合物直接用于人类和动物至关重要,例如在蜂箱内使用杀螨剂治疗蜜蜂身上的瓦螨就是一个极端例子。农药的选择性主要通过生理或生态因素来实现。生理选择性的潜在机制可以基于差异渗透、排泄或代谢、靶位点蛋白亲和力的差异,或两者的结合。基于代谢的选择性既可以通过物种特异性激活来实现,也可以通过解毒来实现。许多杀螨剂,即专门针对螨类和蜱类物种的化合物,具有高度选择性,对昆虫几乎没有效果。这种选择性在已使用数十年的历史参考杀螨剂中得到了记录,在最近开发的化学品中也有体现。对选择性机制的分子见解对于设计专门针对某些害虫的新化合物至关重要。在这篇综述中,我们概述了关于杀螨剂选择性分子机制的已知情况。

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