Identification and pharmacological characterization of the voltage-gated potassium channel Shab in diamondback moth, Plutella xylostella
Identification and pharmacological characterization of the voltage-gated potassium channel Shab in diamondback moth, Plutella xylostella
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DOI：
10.1002/ps.7300
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发表时间：
2022-12-07
影响因子：
4.1
通讯作者：
Liu，Zheming
中科院分区：
文献类型：
--
作者：
Huo，Xiaoyi;Ma，Haihao;Liu，Zheming
背景电压门控钾通道Kv 2是昆虫神经和肌肉中的主要延迟整流器，参与了几个重要的生物学过程，包括动作电位调节、光感受器性能和幼虫运动。它是一个潜在的分子靶标，用于开发一种新的杀虫剂蚊子。然而，关于农业害虫Kv 2通道的研究却很少。结果小菜蛾（Plutella xylostella（L.））中唯一的Kv 2通道α-亚基基因，克隆了PxShab，并分析了其表达谱。PxShab在雌雄成虫蛹期的相对表达量最高，在雌成虫中的相对表达量最低。PxShab在幼虫和成虫头部的表达量最高。然后，PxShab在HEK-293 T细胞系中稳定表达。全细胞膜片钳记录显示外向电流，其电流-电压关系符合典型的延迟整流钾通道。20 μM奎尼丁可有效抑制钾电流，而通道对4-AP不敏感，即使在10 mM时也是如此。结论本研究揭示了PxShab的药理特性，筛选出了几种高效的抑制剂，为PxShab的功能研究奠定了基础，并为设计新型杀虫剂提供了新的思路。© 2022化学工业学会。
BackgroundVoltage‐gated potassium channel Kv2 is the primarily delayed rectifier in insect nerves and muscles involved in several crucial biological processes, including action potential regulation, photoreceptor performance, and larval locomotor. It is a potential molecular target for developing a novel pesticide for mosquitos. However, there are few studies on the Kv2 channel in agricultural pests.ResultsThe only α‐subunit gene of the Kv2 channel inPlutella xylostella(L.),PxShab, was cloned, and its expression profile was analyzed. The relative expression level ofPxShabwas highest in the pupal stage of both sexes and male adults but lowest in female adults. Meanwhile,PxShabhad the highest expression in the head in both larvae and adults. Then, PxShab was stably expressed in the HEK‐293 T cell line. Whole cell patch clamp recordings showed an outward current whose current–voltage relationship conformed to a typical delayed‐rectifier potassium channel. 20 μM quinidine could effectively inhibit the potassium current, while the channel was insensitive to 4‐AP even at 10 mM. Several potential compounds and botanical pesticides were assessed, and carvedilol (IC50= 0.53 μM) and veratrine (IC50= 2.22 μM) had a good inhibitory effect on the channel.ConclusionThis study revealed the pharmacological properties of PxShab and screened out several high potency inhibitors, which laid the foundation for further functional research of PxShab and provides new insight into designing novel insecticides. © 2022 Society of Chemical Industry.