School of Chemical and Environmental Engineering , Shanghai Institute of Technology , Shanghai 201418 , PR China.
Institute of Agro-food Standards and Testing Technologies , Shanghai Academy of Agricultural Science , Shanghai 201403 , PR China.
J Agric Food Chem. 2018 Apr 11;66(14):3644-3650. doi: 10.1021/acs.jafc.8b00197. Epub 2018 Mar 30.
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)propyl]pyridinium 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 (JH) biosynthesis than the lead compound. They significantly inhibited the biosynthesis of JH in vivo following injection. A pest-control application demonstrated that S1 and S3 have larvicidal effects following oral administration (the IC 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.
FGLamide 孤雌生殖抑制素（ASTs）被认为是可能的杀虫剂候选物，尽管它们在体内缺乏效果、快速降解、较差的水溶性和高生产成本，限制了它们在害虫防治中的实际应用。与以前的研究不同，本研究选择 C 末端三肽（FGLa）作为先导化合物。基于 FGLa 的结构-活性关系和对接结果，设计了 5 种非肽 AST 类似物（2-氨基-1-[3-氧代-3-（取代苯胺基）丙基]吡啶𬭩硝酸盐衍生物）。所有的非肽类似物（S1-S5）对昆虫保幼激素（JH）生物合成的抑制作用均强于先导化合物。它们在体内注射后能显著抑制 JH 的生物合成。害虫防治应用表明，S1 和 S3 经口服给药具有杀幼虫作用（IC 值分别为 0.020 和 0.0016 mg/g）。S1 和 S3 具有良好的口服毒性和优异的水溶性，表明它们具有作为杀虫剂防治害虫的巨大潜力。
