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Design, synthesis, insecticidal activities and translocation of amino acid-tralopyril conjugates as vectorizing agrochemicals

文献类型： 外文期刊

作者： Yao, Guangkai 1 ; Han, Shuo 1 ; Wen, Yingjie 1 ; Xiao, Yuyan 1 ; Zhao, Chen 1 ; Xu, Hanhong 1 ;

作者机构： 1.South China Agr Univ, Natl Key Lab Green Pesticide, Key Lab Nat Pesticide & Chem Biol, Guangzhou 510642, Peoples R China

2.South China Agr Univ, Key Lab Nat Pesticide & Chem Biol, Minist Educ, Guangzhou 510642, Peoples R China

3.South China Agr Univ, Coll Plant Protect, Guangzhou 510642, Peoples R China

4.Minist Agr & Rural Affairs, Key Lab South Subtrop Fruit Biol & Genet Resource, Guangzhou, Peoples R China

5.Guangdong Prov Key Lab Trop & Subtrop Fruit Tree R, Guangzhou, Peoples R China

6.Guangdong Acad Agr Sci, Inst Fruit Tree Res, Guangzhou, Peoples R China

关键词： agrochemical vectorization; tralopyril; insecticidal activity; systemicity; proinsecticide

期刊名称：PEST MANAGEMENT SCIENCE （ 影响因子：4.1； 五年影响因子：4.4 ）

ISSN： 1526-498X

年卷期： 2023 年

页码：

收录情况： SCI

摘要： BackgroundConjugating amino acid moieties to active ingredients has been recognized as an effective method for improving the precise targeting of the active form to the specific site. Based on the vectorization strategy, a series of amino acid-tralopyril conjugates were designed and synthesized as novel proinsecticide candidates, with the potential capability of root uptake and translocation to the foliage of crops. ResultsBioassay results showed excellent insecticidal activities of some conjugates, in particular, the conjugates 6b, 6e, and 7e, against the diamondback moth (Plutella xylostella), with equivalent insecticidal activity to chlorfenapyr (CFP). Importantly, conjugate 6e exhibited significantly higher in vivo insecticidal activity against P. xylostella than CFP. Furthermore, the systemic test experiments with Brassica chinensis demonstrated that conjugates 6e and 7e could be transported to the leaves, in contrast to CFP, which remained in the root. ConclusionThis study demonstrated the feasibility of amino acid fragment conjugation as a vectorization strategy for transporting non-systemic insecticides into the leaves of B. chinensis while maintaining in vivo insecticidal activity. The findings also provide insights for subsequent mechanism studies on the uptake and transport of amino acid-insecticide conjugates in plants. (c) 2023 Society of Chemical Industry.

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