文献类型：期刊文献

英文题名：Optical Regulation of Sodium Channels by the Azobenzene Pyrethrins

作者：Fu, Wen[1];Ji, Yunfan[1];Zhang, Yanan[1];Xu, Jiazheng[2];Xu, Zhiping[1];Cheng, Jiagao[1];Li, Zhong[1,3];Shao, Xusheng[1,3,4,5]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China;[2]East China Normal Univ, Lab AI Educ, Shanghai 200062, Peoples R China;[3]East China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China;[4]East China Univ Sci & Technol, Sch Pharm, Shanghai Frontier Sci Res Base Optogenet Tech Cel, Shanghai 200237, Peoples R China;[5]East China Univ Sci & Technol, Engn Res Ctr Pharmaceut Proc Chem, Sch Pharm, Minist Educ, Shanghai 200237, Peoples R China

年份：2022

卷号：2

期号：6

起止页码：1311

外文期刊名：ACS AGRICULTURAL SCIENCE & TECHNOLOGY

收录：WOS:【ESCI(收录号:WOS:000888196900001)】；

基金：This work was financially supported by the National Natural Science Foundation of China (No. 21877039 and 32072441), Innovation Program of Shanghai Municipal Education Commission (2017-01-07-00-02-E00037), and Shanghai Frontiers Science Center of Optogenetic Techniques for Cell Metabolism (Shanghai Municipal Education Commission).

语种：英文

外文关键词：azobenzene; pyrethrins; optical control; insecticidal activities; sodium channel

摘要：Azobenzene compounds exhibit good light stability and have become popular as molecule switches on photopharmacology. Poor photostability hindered the development of pyrethrins until the structural introduction of the phenoxybenzyl group. Herein, strategies of azo-ether replacement and azo-extension are applied to the discovery of novel azobenzene pyrethrins (azo-pyrethrins). We report the optical regulation of sodium channels by the design of azo-pyrethins. The synthesis, photophysicochemical properties, biological activities, and fluorescence analysis were subsequently performed for evaluation of optical control. The results indicate that azo-pyrethins could exhibit good photostability and enable optical control of insecticidal activities against Aphis craccivora and Aedes albopictus larvae. Sf9 cells and DUM neurons were delivered with APY03 or APY11, and fluorescence intensity increases were observed on the cells and neurons after illumination, indicating optical regulation of membrane potential by modulating sodium channels. We expect our work could promote the understanding of spatiotemporal regulation and the mechanism of the sodium channel, providing photochromic ligands in optical control of sodium channels.