数字农科院2.0

Discovery of Natural Products as Multitarget Inhibitors of Insect Chitinolytic Enzymes through High-Throughput Screening

文献类型： 外文期刊

作者： Wenqin Li;Yi Ding;Huitang Qi;Tian Liu;Qing Yang*

作者机构：

关键词： chitinase;inhibitor;insecticide;multitarget;natural product

期刊名称： Journal of Agricultural and Food Chemistry

ISSN： 0021-8561

年卷期： 2021 年 69.0 卷 37.0 期

页码：

收录情况： JCR（2021版） ; EI（2021版）

摘要： Small-molecule inhibitors of insect chitinolytic enzymes are potential insecticides. However, the reported inhibitors that target one enzyme usually exhibit unsatisfactory bioactivity. On the basis of the multitarget strategy, we performed a high-throughput screening of a natural product library to find insecticide leads against four chitinolytic enzymes from the Asian corn borer Ostrinia furnacalis (OfChtI, OfChtII, OfChi-h, and OfHex1). Several phytochemicals were discovered to be multitarget inhibitors of these enzymes and were predicted to occupy the -1 substrate-binding subsite and engage in polar interactions with catalytically important residues. Shikonin and wogonin, which had good inhibitory activities toward all four enzymes, also exhibited significant insecticidal activities against lepidopteran agricultural pests. This study provides the first example of using a multitarget high-throughput screening strategy to exploit natural products as insecticide leads against chitin biodegradation during insect molting.

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