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Structure-Based Discovery of Nonpeptide Allatostatin Analogues for Pest Control

文献类型： 外文期刊

作者： Huang, Shan-shan 1 ; Chen, Shan-shan 2 ; Zhang, Hong-ling 1 ; Yang, Han 1 ; Yang, Hui-juan 1 ; Ren, Yu-jie 1 ; Kai, Zh 1 ;

作者机构： 1.Shanghai Inst Technol, Sch Chem & Environm Engn, Shanghai 201418, Peoples R China

2.Shanghai Acad Agr Sci, Inst Agrofood Stand & Testing Technol, Shanghai 201403, Peoples R China

关键词： allatostatin; juvenile hormone; nonpeptide analogues; oral toxicity; cockroach

期刊名称：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY （ 影响因子：5.279； 五年影响因子：5.269 ）

ISSN： 0021-8561

年卷期： 2018 年 66 卷 14 期

页码：

收录情况： SCI

摘要： FGLamide allatostatins (ASTs) are regarded as possible insecticide candidates, although their lack of in vivo effects, rapid degradation, poor water solubility, and high production costs preclude their practical use in pest control. In contrast to previous research, the C-terminal tripeptide (FGLa) was selected as the lead compound in this study. Five nonpeptide AST analogues (2-amino-1[3-oxo-3-(substituted-anilino)propylipyridinium nitrate derivatives) were designed on the basis of the structure-activity relationship and docking results of FGLa. All of the nonpeptide analogues (S1-S5) were more potent against juvenile-hormone OH) biosynthesis than the lead compound. They significantly inhibited the biosynthesis of JH in vivo following injection. A pest-control application demonstrated that Si and S3 have larvicidal effects following oral administration (the IC50 values were 0.020 and 0.0016 mg/g, respectively). The good oral toxicities and excellent water solubilities of S1 and S3 suggest that they have considerable potential as insecticides for pest management.

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