Synthesis, Translocation, and Biological Activity of an Artificial Glucosinolate with a Fipronil-Based Aglycone as a Vectorizing Agrochemical
文献类型： 外文期刊
作者： Wen, Yingjie 1 ; Jiang, Xunyuan 3 ; Li, Dehong 1 ; Yu, Ye 1 ; Ou, Ziyue 1 ; Wang, Jiali 1 ; Wei, Jiaqi 1 ; Lin, Fei 1 ; Xu, Hanhong 1 ;
作者机构： 1.South China Agr Univ, State Key Lab Green Pesticide, Guangzhou 510640, Peoples R China
2.South China Agr Univ, Coll Plant Protect, Key Lab Nat Pesticide & Chem Biol, Minist Educ, Guangzhou 510640, Peoples R China
3.Guangdong Acad Agr Sci, Inst Qual Stand & Monitoring Technol Agroprod, Guangdong Prov Key Lab Qual & Safety Risk Assessme, Guangzhou 510640, Peoples R China
4.Guangdong Acad Agr Sci, Inst Fruit Tree Res, Guangzhou 510640, Peoples R China
5.Minist Agr & Rural Affairs, Key Lab South Subtrop Fruit Biol & Genet Resource, Guangdong Prov Key Lab Sci & Technol Res Fruit Tre, Guangzhou 510640, Peoples R China
关键词： glucosinolates; glucosinolate transporter; systemic pesticide; uptake
期刊名称：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY （ 影响因子：6.2； 五年影响因子：6.4 ）
ISSN： 0021-8561
年卷期： 2025 年 73 卷 24 期
页码：
收录情况： SCI
摘要： The conversion of nonsystemic pesticides into systemic agents can enhance their efficacy, with plant transporters representing a promising strategy. Glucosinolate transporters (GTR1/GTR2) mediate glucosinolate uptake and transport but remain unexplored for pesticide uptake. In this study, we synthesized an artificial glucosinolate (FIP-GSL) with fipronil as the substituent group. Xenopus oocyte assays showed that GTR1/GTR2 mediated FIP-GSL uptake in a proton-dependent manner. Molecular docking revealed conserved salt-bridge interactions between the sulfate group of FIP-GSL and key residues (Lys79/Arg196 in GTR1; Lys61/Arg180 in GTR2), which were essential for proton-coupled transport. In Arabidopsis, FIP-GSL exhibited phloem-mediated translocation in wild-type plants, but this translocation was reduced in the gtr1, gtr2, and gtr1gtr2 mutants. Biological assays revealed that although the direct activity of FIP-GSL was lower than that of fipronil, its systemic efficacy was significantly enhanced. Moreover, FIP-GSL displayed substantially reduced toxicity to bees. These findings demonstrate that exploiting GTR1 and GTR2 to enhance pesticide uptake and translocation could offer a promising strategy for improving the systemic activity of agrochemicals.
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