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Lynamicin B通过作为鳞翅目特异性几丁质酶抑制剂而成为一种潜在的杀虫剂。

Lynamicin B is a Potential Pesticide by Acting as a Lepidoptera-Exclusive Chitinase Inhibitor.

作者信息

Lu Qiong, Xu Liping, Liu Lin, Zhou Yong, Liu Tian, Song Yongxiang, Ju Jianhua, Yang Qing

机构信息

School of Bioengineering, Dalian University of Technology, Dalian 116024, China.

CAS Key Laboratory of Tropical Marine Bio-resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, RNAM Center for Marine Microbiology, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, China.

出版信息

J Agric Food Chem. 2021 Dec 1;69(47):14086-14091. doi: 10.1021/acs.jafc.1c05385. Epub 2021 Nov 19.

Abstract

Insect group h chitinase is a promising target for designing non-target safe pesticides in that it is exclusively distributed in lepidopteran insects, over 80% of which are agricultural pests. In this work, lynamicin B was discovered to be an inhibitor of Chi-h, the group h chitinase from the lepidopteran pest . Lynamicin B was revealed to competitively inhibit Chi-h with a value of 8.76 μM and does not significantly inhibit other chitinases. The co-crystal structure of lynamicin B and Chi-h revealed that the dichloroindolyl group of lynamicin B occupies an unexplored pocket below subsites +1 and +2 of the substrate-binding cleft, which is vital for its selectivity. Feeding experiments demonstrated that lynamicin B exhibited high insecticidal activities against other lepidopteran pests and besides . Moreover, lynamicin B did not affect , a natural enemy of . This study provides a natural-derived potent pesticide for the control of lepidopteran pests, leaving its natural enemy unaffected.

摘要

昆虫H组几丁质酶是设计非靶标安全农药的一个有前景的靶点,因为它仅分布在鳞翅目昆虫中,其中超过80%是农业害虫。在这项研究中,发现lynamicin B是鳞翅目害虫H组几丁质酶Chi-h的一种抑制剂。研究表明,lynamicin B对Chi-h具有竞争性抑制作用,IC50值为8.76 μM,且对其他几丁质酶无显著抑制作用。lynamicin B与Chi-h的共晶体结构表明,lynamicin B的二氯吲哚基团占据了底物结合裂隙亚位点+1和+2下方一个未被探索的口袋,这对其选择性至关重要。喂食实验表明,lynamicin B除了对棉铃虫和烟芽夜蛾外,对其他鳞翅目害虫也表现出高杀虫活性。此外,lynamicin B对棉铃虫的天敌草蛉没有影响。本研究为防治鳞翅目害虫提供了一种天然来源的高效农药,且不会影响其天敌。

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