Synthesis, bioactivity and functional evaluation of linker-modified allatostatin analogs as potential insect growth regulators
Synthesis, bioactivity and functional evaluation of linker-modified allatostatin analogs as potential insect growth regulators
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DOI：
10.1016/j.cclet.2016.02.010
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发表时间：
2016-04
影响因子：
9.1
通讯作者：
Tobe Stephen S.
中科院分区：
文献类型：
--
作者：
Wu Xiao-Qing;Huang Juan;Wang Mei-Zi;Zhang Zhe;Li Xin-Lu;Yang Xin-Ling;Tobe Stephen S.
昆虫生长调节剂在害虫综合治理战略中发挥着重要作用。FGLa-allatostatins （ast）是一类能在体外抑制斑点双翅虫异形体（CA）合成幼体激素（JH）的神经肽，被认为是昆虫生长调节剂的候选物质。为了寻找新的潜在的模拟物，探索连接体长度对抑制JH生物合成的影响，我们通过修饰K24的连接体合成了一系列AST类似物，在vitroin中发现这些类似物对JH生物合成有显著的影响。功能评价表明，所有的目标化合物都能激活dippu - astr，只是活性不同。具有最长连接体（n= 5）的类似物L6不仅在体外和体内对JH生物合成有良好的抑制作用，而且在抑制基底卵母细胞生长方面也有良好的活性。结构-活性关系（SAR）研究表明，较长的连接体对活性的贡献更大。
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) ofDiploptera 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 biosynthesisin vitroin our previous study. Functional evaluation demonstrated that all the target compounds can activate theDippu-AstR, albeit with different potencies. Analog L6 with the longest linker (n= 5), exhibited not only a promising effect on inhibition of JH biosynthesis bothin vitroandin vivo, but also good activity in inhibiting basal oocyte growth. Structure–activity relationships (SAR) studies showed that longer linkers provided greater contribution to activity.
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