Huang Ling, Huang Lin-Yu, Shan Lian-Hai, Gao Feng, Zheng Ling-Li, Xu Jin-Bu
Department of Pharmacy, The First Affiliated Hospital of Chengdu Medical College, Chengdu 610500, People's Republic of China.
Sichuan Engineering Research Center for Biomimetic Synthesis of Natural Drugs, School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, Sichuan, People's Republic of China.
ACS Omega. 2024 Aug 27;9(36):38169-38179. doi: 10.1021/acsomega.4c05568. eCollection 2024 Sep 10.
Introducing a sulfur atom into active agricultural molecules is an important strategy for pesticide development. Matrine, an environmentally friendly botanical pesticide, has the advantage of being easily degraded and has drawn attention in the agricultural field. To explore the novel matrine-type pesticides, in this study, we designed and synthesized 13/14-arylthioether matrine derivatives by introducing various aryl sulfide motifs into bioactive matrine. Most of the synthesized arylthioether matrines exhibited good antifeedant activity against . Among them, compound showed the best antifeedant effect with an EC value of 0.038 mg/mL, which is approximately 125-fold more activity than matrine and reached the activity level of commercial standard azadirachtin A. Furthermore, compound exhibited an inhibitory effect on antifeedant-related enzyme carboxylesterase (CarE) from . In short, the high activity of arylthioether matrines offers new insights into developing new antifeedants.
将硫原子引入活性农业分子是农药开发的一项重要策略。苦参碱是一种环境友好型植物源农药，具有易于降解的优点，已在农业领域引起关注。为了探索新型苦参碱类农药，在本研究中，我们通过将各种芳基硫醚基序引入具有生物活性的苦参碱中，设计并合成了13/14-芳硫基苦参碱衍生物。大多数合成的芳硫基苦参碱对……表现出良好的拒食活性。其中，化合物……表现出最佳的拒食效果，EC值为0.038 mg/mL，其活性约为苦参碱的125倍，达到了商业标准印楝素A的活性水平。此外，化合物……对来自……的拒食相关酶羧酸酯酶（CarE）表现出抑制作用。简而言之，芳硫基苦参碱的高活性为开发新型拒食剂提供了新的思路。
