Synthesis, bioactivity and functional evaluation of linker-modified allatostatin analogs as potential insect growth regulators  

作　　者：Xiao-Qing Wu Juan Huang Mei-Zi Wang Zhe Zhang Xin-Lu Li Xin-Ling Yang Stephen S.Tobe 

机构地区：[1]Department of Applied Chemistry, College of Science, China Agricultural University [2]Department of Cell and Systems Biology, University of Toronto

出　　处：《Chinese Chemical Letters》2016年第4期559-562,共4页中国化学快报（英文版）

基　　金：supported by the National Natural Science Foundation of China (No. 21372257);the National Basic Research Program of China (973 Program, No. 2010CB126104);the Natural Sciences and Engineering Research Council of Canada;supported by China Scholarship Council (CSC) to study in the laboratory of SST at University of Toronto,Canada

摘　　要：Insect growth regulators play an important role in integrated pest management strategies.The FGLa–allatostatins（ASTs）are a family of neuropeptides that can inhibit juvenile hormone（JH）biosynthesis by the corpora allata（CA）of Diploptera punctata in vitro,are regarded as insect growth regulator candidates.In the search for new potential mimics and to explore the effect of linker length on inhibiting JH biosynthesis,a series of AST analogs were synthesized by modifying the linker of K24,which was found to have a significant effect on JH biosynthesis in vitro in our previous study.Functional evaluation demonstrated that all the target compounds can activate the Dippu-Ast R,albeit with different potencies.Analog L6 with the longest linker（n=5）,exhibited not only a promising effect on inhibition of JH biosynthesis both in vitro and in vivo,but also good activity in inhibiting basal oocyte growth.Structure–activity relationships（SAR）studies showed that longer linkers provided greater contribution to activity.Insect growth regulators play an important role in integrated pest management strategies.The FGLa–allatostatins（ASTs）are a family of neuropeptides that can inhibit juvenile hormone（JH）biosynthesis by the corpora allata（CA）of Diploptera punctata in vitro,are regarded as insect growth regulator candidates.In the search for new potential mimics and to explore the effect of linker length on inhibiting JH biosynthesis,a series of AST analogs were synthesized by modifying the linker of K24,which was found to have a significant effect on JH biosynthesis in vitro in our previous study.Functional evaluation demonstrated that all the target compounds can activate the Dippu-Ast R,albeit with different potencies.Analog L6 with the longest linker（n=5）,exhibited not only a promising effect on inhibition of JH biosynthesis both in vitro and in vivo,but also good activity in inhibiting basal oocyte growth.Structure–activity relationships（SAR）studies showed that longer linkers provided greater contribution to activity.

关 键 词：ALLATOSTATIN Insect growth regulators Juvenile hormone ANALOGS Dippu-Ast receptor 

分 类 号：TQ453[化学工程—农药化工]