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基于昆虫糖基水解酶的抑制剂筛选
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摘要
几丁质作为昆虫表皮的重要组成部分,在昆虫的生长发育特别是周期性蜕皮过程中具有重要的作用。昆虫体内存在非常高效的几丁质降解系统,包含有大量的糖基水解酶负责其蜕皮过程,其中属于糖基水解酶20家族的N-乙酰己糖胺酶Hex1及18家族的几丁质酶h发挥了极为重要的作用,因此被认为是潜在的绿色农药靶标。本文以来源于亚洲玉米螟的N-乙酰己糖胺酶OfHex1及几丁质酶OfChi-h为研究对象,从微生物代谢库中筛选获得了抑制剂283和312,两者对OfHex1及OfChi-h均表现出较高的抑制活性和选择性。本研究工作为针对昆虫蜕皮过程的绿色农药开发提供了先导化合物。
Chitin,plays an important role in the molting,is an essential part of the insect cuticle.An efficient chitin degradation system which containing a large number of glycosyl hydrolases responseing molting is explored.Among all the glycosyl hydrolases,P-acetylglucosaminidases and chitinase h,which belong to family 20 and family 18 respectively,are considered to be extremely important and as a potential target for developing green pesticide.Here,an inhibitor screening of OfHex1 and OfChi-h from Ostriniafurnacalis is performed and two microbial metabolites 283 and 312 which show both high inhibitory activity and selectivity toward OfHex 1 and OfChi-h are obtained.The work here provides lead compounds for the green pesticide development.
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