文献类型：期刊文献

英文题名：Optical Control of Insect Behavior and Receptors with Azobenzene-Bridged Fipronil and Imidacloprid

作者：Fu, Wen[1];Sheng, Zhubo[1];Qiao, Zhi[1];Xu, Zhiping[1];Li, Meng[5];Guan, Ying[5];Li, Zhong[1,2];Shao, Xusheng[1,2,3,4]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China;[3]East China Univ Sci & Technol, Sch Pharm, Shanghai Frontier Sci Res Base Optogenet Tech Cell, Shanghai 200237, Peoples R China;[4]East China Univ Sci & Technol, Sch Pharm, Engn Res Ctr Pharmaceut Proc Chem, Minist Educ, Shanghai 200237, Peoples R China;[5]Joint Inst Tobacco & Hlth, Kunming 650202, Yunnan, Peoples R China

年份：2024

卷号：72

期号：22

起止页码：12469

外文期刊名：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

收录：;EI(收录号：20242216152428);WOS:【SCI-EXPANDED(收录号:WOS:001228934600001)】；

基金：This work was financially supported by National Natural Science Foundation of China (No. 21877039, No. 32072441), National Key Research and Development Program of China (2018YFD0200100), Innovation Program of Shanghai Municipal Education Commission (2017-01-07-00-02-E00037), Tobacco and Health funding program (No.2022539200340111), Shanghai Frontiers Science Center of Optogenetic Techniques for Cell Metabolism (Shanghai Municipal Education Commission).

语种：英文

外文关键词：azobenzene bridge; multiphoton; insect receptorand behavior; spatiotemporal; regulation

摘要：Photopharmacology can be implemented in a way of regulating drug activities by light-controlling the molecular configuations. Three photochromic ligands (PCLs) that bind on one or two sites of GABARs and nAChRs were reported here. These multiphoton PCLs, including FIP-AB-FIP, IMI-AB-FIP, and IMI-AB-IMI, are constructed with an azobenzene (AB) bridge that covalently connects two fipronil (FIP) and imidacloprid (IMI) molecules. Interestingly, the three PCLs as well as FIP and IMI showed great insecticidal activities against Aedes albopictus larvae and Aphis craccivora. IMI-AB-FIP in both trans/cis isomers can be reversibly interconverted depending on light, accompanied by insecticidal activity decrease or increase by 1.5-2.3 folds. In addition, IMI-AB-FIP displayed synergistic effects against A. craccivora (LC50, IMI-AB-FIP = 14.84-22.10 mu M, LC50, IMI-AB-IMI = 210.52-266.63 mu M, LC50, and FIP-AB-FIP = 36.25-51.04 mu M), mainly resulting from a conceivable reason for simultaneous targeting on both GABARs and nAChRs. Furthermore, modulations of wiggler-swimming behaviors and cockroach neuron function were conducted and the results indirectly demonstrated the ligand-receptor interactions. In other words, real-time regulations of receptors and insect behaviors can be spatiotemporally achieved by our two-photon PCLs using light.