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

引用本文: Xiao-Qing Wu, Juan Huang, Mei-Zi Wang, Zhe Zhang, Xin-Lu Li, Xin-Ling Yang, Stephen S. Tobe. Synthesis, bioactivity and functional evaluation of linker-modified allatostatin analogs as potential insect growth regulators[J]. Chinese Chemical Letters, 2016, 27(4): 559-562. shu

Citation: Xiao-Qing Wu, Juan Huang, Mei-Zi Wang, Zhe Zhang, Xin-Lu Li, Xin-Ling Yang, Stephen S. Tobe. Synthesis, bioactivity and functional evaluation of linker-modified allatostatin analogs as potential insect growth regulators[J]. Chinese Chemical Letters, 2016, 27(4): 559-562. shu

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

a Department of Applied Chemistry, College of Science, China Agricultural University, Beijing 100193, China;
b Department of Cell and Systems Biology, University of Toronto, Toronto, ON, Canada M5S 3G5
基金项目:
This study was financially supported by the National Natural Science Foundation of China (No. 21372257), the National Basic Research Program of China (973 Program, No. 2010CB126104) and theNatural Sciences and Engineering Research Council of 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-AstR, 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:

English

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

a Department of Applied Chemistry, College of Science, China Agricultural University, Beijing 100193, China;
b Department of Cell and Systems Biology, University of Toronto, Toronto, ON, Canada M5S 3G5
Received Date: 04 January 2016
Revised Date: 23 January 2016
Available Online: 02 March 2016
Fund Project:
This study was financially supported by the National Natural Science Foundation of China (No. 21372257), the National Basic Research Program of China (973 Program, No. 2010CB126104) and theNatural Sciences and Engineering Research Council of Canada.

Abstract: 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-AstR, 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.

Key words:

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

English

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

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

English

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

CCS Chemistry：嵌段共聚物自组装成 “三明治”二维有机材料，实现纳米级压力传感功能

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