Lu Qiong, Xu Liping, Liu Lin, Zhou Yong, Liu Tian, Song Yongxiang, Ju Jianhua, Yang Qing
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.
J Agric Food Chem. 2021 Dec 1;69(47):14086-14091. doi: 10.1021/acs.jafc.1c05385. Epub 2021 Nov 19.
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.
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。
