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计算方法在农药靶标位点及抗性机制分析中的应用

Application of computational methods in the analysis of pesticide target-site and resistance mechanisms.

作者信息

Banba Shinichi

机构信息

Research and Development Division, Mitsui Chemicals Agro, Inc., 1144, Togo, Mobara, Chiba 297-0017, Japan.

出版信息

J Pestic Sci. 2021 Aug 20;46(3):283-289. doi: 10.1584/jpestics.J21-01.

DOI:10.1584/jpestics.J21-01
PMID:34566463
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8422262/
Abstract

-diamide insecticides including broflanilide have a high insecticidal activity by acting on RDL GABA receptors. Both membrane potential assays and docking studies suggest that the target site of -diamides is different from that of conventional noncompetitive inhibitors, such as fipronil. In fact, -diamides are effective against cyclodiene- and fipronil-resistant pests that carry target-site mutations. Dinotefuran uniquely possesses a tetrahydrofuran ring, whereas other neonicotinoids possess aromatic rings. Moreover, dinotefuran has been reported to be effective against imidacloprid-resistant strains. A docking study predicted the weak binding of dinotefuran to cytochrome P450s which are associated with imidacloprid resistance. Metabolic assays revealed that dinotefuran was not metabolized by these cytochrome P450s. These findings suggest that the lack of metabolic activity of P450s against dinotefuran causes a low level of cross-resistance.

摘要

包括溴虫氟苯双酰胺在内的双酰胺类杀虫剂通过作用于RDL GABA受体具有很高的杀虫活性。膜电位测定和对接研究均表明，双酰胺类的作用靶位点与传统非竞争性抑制剂（如氟虫腈）不同。事实上，双酰胺类对携带靶位点突变的环二烯类和氟虫腈抗性害虫有效。呋虫胺独特地拥有一个四氢呋喃环，而其他新烟碱类则拥有芳香环。此外，据报道呋虫胺对吡虫啉抗性品系有效。一项对接研究预测呋虫胺与与吡虫啉抗性相关的细胞色素P450s的结合较弱。代谢试验表明，这些细胞色素P450s不会使呋虫胺代谢。这些发现表明，P450s对呋虫胺缺乏代谢活性导致了低水平的交叉抗性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/a9e9e603bdce/jps-46-3-J21-01-figure09.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/6c5280132c3a/jps-46-3-J21-01-figure01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/fdee31428f99/jps-46-3-J21-01-figure02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/8fed4a76d01d/jps-46-3-J21-01-figure03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/bf3747509134/jps-46-3-J21-01-figure04.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/c8e1a492920e/jps-46-3-J21-01-figure05.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/a7ebf289fb29/jps-46-3-J21-01-figure06.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/aaf2e5c2e3ea/jps-46-3-J21-01-figure07.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/02f9ce1be60a/jps-46-3-J21-01-figure08.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/a9e9e603bdce/jps-46-3-J21-01-figure09.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/6c5280132c3a/jps-46-3-J21-01-figure01.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/fdee31428f99/jps-46-3-J21-01-figure02.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/8fed4a76d01d/jps-46-3-J21-01-figure03.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/bf3747509134/jps-46-3-J21-01-figure04.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/c8e1a492920e/jps-46-3-J21-01-figure05.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/a7ebf289fb29/jps-46-3-J21-01-figure06.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/aaf2e5c2e3ea/jps-46-3-J21-01-figure07.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/02f9ce1be60a/jps-46-3-J21-01-figure08.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ffd4/8422262/a9e9e603bdce/jps-46-3-J21-01-figure09.jpg

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