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

第一作者: Wen, Yingjie

作者: Wen, Yingjie;Li, Dehong;Yu, Ye;Ou, Ziyue;Wang, Jiali;Wei, Jiaqi;Lin, Fei;Xu, Hanhong;Wen, Yingjie;Li, Dehong;Yu, Ye;Ou, Ziyue;Wang, Jiali;Wei, Jiaqi;Lin, Fei;Xu, Hanhong;Jiang, Xunyuan;Wen, Yingjie;Wen, Yingjie

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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

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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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