新烟碱类杀虫剂吡虫啉和噻虫嗪的代谢研究进展  

Research progresses on the metabolism of neonicotinoids imidacloprid and thiamethoxam

作　　者：范银君[1] 史雪岩[1] 高希武[1] 

机构地区：[1]中国农业大学农学与生物技术学院,北京100193

出　　处：《农药学学报》2012年第6期587-596,共10页Chinese Journal of Pesticide Science

基　　金：农业部公益性行业科技专项(200903033);国家自然科学基金(30771426);教育部"新世纪优秀人才支持计划"(NCET-06-0113)

摘　　要：对新烟碱类杀虫剂吡虫啉和噻虫嗪的化学结构特点及代谢研究进展进行了综述,重点对其在哺乳动物、植物和昆虫体内的代谢途径及相关的生物代谢酶进行了阐述。吡虫啉和噻虫嗪在环境中可被动物、植物、微生物及昆虫所代谢,与其生物代谢相关的酶主要是微粒体细胞色素P450同工酶和醛氧化酶,其中,P450同工酶可催化吡虫啉和噻虫嗪发生羟基化、去饱和、脱烷基、硝基还原等代谢反应,而醛氧化酶主要催化其硝基部分的还原。吡虫啉和噻虫嗪经过代谢后其生物活性通常有所降低,但也有部分代谢产物的活性反而升高,增加了其对昆虫的毒性以及对非靶标生物的风险。明确吡虫啉和噻虫嗪的代谢途径、代谢产物及其生物活性,对于了解新烟碱类杀虫剂的代谢机理,以及安全有效地使用该类杀虫剂具有重要意义。The structure characteristics of neonicotinoids insecticides imidacloprid（IMI）and thiamethoxam（TMX）and the research progresses on the metabolisms of IMI and TMX in mammals,plants and insects,especially the metabolic pathway and the relative major enzymes in the metabolism of IMI and TMX are reviewed.IMI and TMX could be gradually metabolized by mammals,plants,microorganisms and insects in the environment.Microsomal cytochrome 450s（CYP450s）and cytosolic aldehyde oxidase（AOX）are the major enzymes involved in the metabolism of IMI and TMX.CYP450s isozymes are responsible for the hydroxylation,desaturation,dealkylation and nitro reduction of imidacloprid and thiamethoxam,while AOX reduced the nitro group of IMI and TMX.The biological activities of some metabolites of IMI and TMX are usually lower than that of native IMI and TMX,but in some cases,IMI and TMX act as proinsecticides,which could be metabolized to more potent nicotinic agonists.The activated metabolites of IMI and TMX would improve the insecticidal activity against the pest insects and the risks for non-target organisms.Identification of the metabolic pathway,metabolites and activities of neonicotinoids are important for understanding the toxicity mechanism of neonicotinoids metabolism,as well as the safe and efficient application neonicotinoids insecticides.

关 键 词：新烟碱类杀虫剂 吡虫啉 噻虫嗪 代谢 细胞色素P450同工酶 醛氧化酶 

分 类 号：S482.3[农业科学—农药学] S481.1[农业科学—植物保护]