Azobenzene-Semicarbazone Enables Optical Control of Insect Sodium Channels and Behavior
作者:Zhi Qiao、Wen Fu、Yongchao Zhang、Ruijia Chen、Zhiping Xu、Zhong Li、Xusheng Shao
DOI:10.1021/acs.jafc.1c06404
日期:2021.12.29
Photopharmacology uses molecular photoswitches to establish control over the action of bioactive molecules. The application of photopharmacology in the research of invertebrate sodium channels has not been investigated. Here we report several photochromic ligands of metaflumizone. One ligand, termed ABM04, underwent reversible trans–cis isomerization under ultraviolet or blue light irradiation. cis-ABM04
光药理学使用分子光开关来控制生物活性分子的作用。光药理学在无脊椎动物钠通道研究中的应用尚无研究。在这里我们报告了氰氟虫腙的几种光致变色配体。一种称为ABM04 的配体在紫外线或蓝光照射下经历了可逆的反式-顺式异构化。cis -ABM04对蚊子幼虫具有优异的杀幼虫活性,LC 50值为 4.39 μM,对Mythimna separata具有杀虫活性,LC 50值为 7.19 μM。然而,反ABM04未发现具有生物活性。ABM04 (10 μM) 可以诱导背侧未配对的正中神经元去极化,并使蚊子幼虫行为的实时光调节成为可能。首次实现了对无脊椎动物钠通道的精准调控,为无脊椎动物钠通道的基础精准研究提供了新的思路。