海藻糖酶结构及其抑制剂的农用活性研究进展  

Trehalase structures and agriculture bioactivities of its inhibitors:a review

作　　者：师东梅 蒋志洋 邹雪君 黄家兴[1] 段红霞[1] SHI Dongmei;JIANG Zhiyang;ZOU Xuejun;HUANG Jiaxing;DUAN Hongxia(Innovation Center of Pesticide Research,Department of Applied Chemistry,College of Science,China Agricultural University,Beijing 100193,China)

机构地区：[1]中国农业大学理学院应用化学系农药创新研究中心,北京100193

出　　处：《农药学学报》2022年第5期1017-1033,共17页Chinese Journal of Pesticide Science

基　　金：植物病虫害生物学国家重点实验室开放基金(SKLOF202107);国家自然科学基金(32172445,31972289).

摘　　要：海藻糖是一种非还原性二糖,在昆虫、真菌等有害生物体内参与能量代谢、逆境恢复、几丁质合成等过程。海藻糖酶(EC 3.2.1.28)由于其对海藻糖代谢及其含量调控具有重要作用,且在农业有害生物和哺乳动物体内存在功能差异,已成为开发新型农用化学品的安全型候选靶标。本文对海藻糖酶的晶体结构、海藻糖酶与底物/抑制剂的互作机制研究进展进行了综述;同时对具有农用活性的海藻糖酶抑制剂,如井冈霉素、天然产物salbostatin和trehazolin及其合成类似物、脱氧野尻霉素及其合成类似物、天然生物碱及其合成类似物以及胡椒碱及其类似物的研究进展进行了概述,并重点论述了以胡椒碱为骨架的化合物在农业有害生物防治上的应用。本综述可为靶向海藻糖酶结构进行新型胡椒碱类结构的农用化学品设计与发现提供参考。Trehalose is a non-reducing disaccharide that has a variety of biological functions in insects or fungi such as participating in energy metabolism,recovery from stress,and chitin synthesis.Trehalase(EC 3.2.1.28)has become a safe candidate target for the development of novel agrochemicals due to its important roles in regulating the metabolism and the content of trehalose,as well as its functional differences between pests and mammals.In this review,the crystal structures of trehalase and its interaction mechanism with inhibitors are summarized.Meanwhile,the research progress of trehalase inhibitors in agriculture is overviewed including validamycin,natural products salbostatin and trehazolin,deoxynojirimycin,natural alkaloids,piperine,and their corresponding synthetic analogues.In addition,the application of piperine-based compounds in the control of plant diseases or pests is highlighted.This review would provide a reference for the design and the discovery of novel piperinebased agrochemicals targeting the structure of trehalase.

关 键 词：海藻糖酶 海藻糖酶抑制剂 胡椒碱类化合物 农用生物活性 合理设计 

分 类 号：TQ450.1[化学工程—农药化工]