Effects of the novel acaricide acynonapyr on the calcium-activated potassium channel

IF 4.2 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology Pub Date : 2024-08-08 DOI:10.1016/j.pestbp.2024.106074

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Abstract

Resistance to insecticides and acaricides is a major impediment to effectively controlling insect pests worldwide. These pests include the two-spotted spider mite Tetranychus urticae (T. urticae), which exists globally. This polyphagous herbivore causes major agricultural problems and can develop resistance to the agents above. Therefore, the continuous development of acaricides with new modes of action is important to circumvent the resistance of insects to pesticides. Acynonapyr is a novel class of acaricides containing an azabicyclo ring. In this study, we determined the activity of acynonapyr and its analogs on calcium-activated potassium (K_Ca2) channels in two-spotted spider mites using electrophysiological techniques (patch-clamp). We also examined their acaricidal efficacy against mites in the laboratory. The acynonapyr and analogs blocked T. urticae K_Ca2 (TurK_Ca2) channels in a concentration-dependent manner. A comparison of acaricidal activity against T. urticae with inhibitory activity against TurK_Ca2 revealed that TurK_Ca2 channels are the primary toxicological targets. Finally, we examined the effect of acynonapyr on Homo sapiens K_Ca2 (HsaK_Ca2.2) channels and demonstrated that the compound at 10 μM had a limited effect on the activity of this channel.

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新型杀螨剂炔草酯对钙激活钾通道的影响

对杀虫剂和杀螨剂的抗药性是有效控制全球害虫的主要障碍。这些害虫包括存在于全球的双斑蜘蛛螨（Tetranychus urticae，T. urticae）。这种多食性食草动物会造成严重的农业问题，而且会对上述药剂产生抗药性。因此，不断开发具有新作用模式的杀螨剂对于避免昆虫对杀虫剂产生抗药性非常重要。炔草酯是一类含有氮杂双环的新型杀螨剂。在这项研究中，我们利用电生理技术（膜片钳）测定了炔草酯及其类似物对二斑蛛螨体内钙激活钾（KCa2）通道的活性。我们还在实验室中检测了它们对螨虫的杀螨功效。炔草酯及其类似物以浓度依赖性的方式阻断了T. urticae KCa2（TurKCa2）通道。通过比较对荨麻螨的杀螨活性和对 TurKCa2 的抑制活性，我们发现 TurKCa2 通道是主要的毒性靶标。最后，我们研究了炔草酯对智人 KCa2（HsaKCa2.2）通道的影响，结果表明 10 μM 的化合物对该通道的活性影响有限。

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来源期刊

Pesticide Biochemistry and Physiology 生物-昆虫学

CiteScore

7.00

自引率

8.50%

发文量

238

审稿时长

4.2 months

期刊介绍： Pesticide Biochemistry and Physiology publishes original scientific articles pertaining to the mode of action of plant protection agents such as insecticides, fungicides, herbicides, and similar compounds, including nonlethal pest control agents, biosynthesis of pheromones, hormones, and plant resistance agents. Manuscripts may include a biochemical, physiological, or molecular study for an understanding of comparative toxicology or selective toxicity of both target and nontarget organisms. Particular interest will be given to studies on the molecular biology of pest control, toxicology, and pesticide resistance. Research Areas Emphasized Include the Biochemistry and Physiology of: • Comparative toxicity • Mode of action • Pathophysiology • Plant growth regulators • Resistance • Other effects of pesticides on both parasites and hosts.