缩氨基硫脲化合物的合成及对菜青虫酚氧化酶抑制作用研究  

Study on the Synthesis and Inhibitory Effects of Thiosemicarbazones on Phenoloxidase from Pieres rapae L.

作　　者：李智聪[1] 马素娟[1] 潘志针[1] 杨美花[1] 秦江[1] 陈清西[1,2] 

机构地区：[1]厦门大学生命科学学院,细胞生物学与肿瘤细胞工程教育部重点实验室,福建厦门361005 [2]厦门大学化学生物学福建省重点实验室,福建厦门361005

出　　处：《厦门大学学报（自然科学版）》2009年第5期623-626,共4页Journal of Xiamen University：Natural Science

基　　金：国家自然科学基金(30570408,20832005);福建省重点科技项目(2007N0051)资助

摘　　要：菜青虫是危害农作物的主要害虫,酚氧化酶在昆虫的生长发育过程中起着重要的调节作用,高效的酚氧化酶抑制剂对于发展新型"环境友好"杀虫剂有着重要的意义.设计合成了4种缩氨基硫脲类化合物,采用红外光谱、质谱和核磁共振谱对其进行结构鉴定,进一步研究了它们对菜青虫酚氧化酶的抑制作用,结果表明,4种化合物均有显著的抑制作用,其半抑制率IC50分别为2.88,0.93,3.60和0.22μmol/L,有可能进一步开发成为以酚氧化酶为靶点的新型生物农药.同时,为基于缩氨基硫脲母核的酚氧化酶抑制剂的设计提供了数据基础.Pieres rapae L. was a kind of insects harmful to vegetables. Phenoloxidase （PO） is responsible for enzymatic browning during the growth of the insects. It also is involved in the defense reaction and has some certain relation with the immune condition of the insects, and effective PO inhibitors are of great values in developing new,environment friendly pesticide. In this study, four thiosemicarbazone compounds were synthesized and indentified by IR, ESI-MS and NMR. Furthermore, their inhibitory effects on PO from Pieres rapae L. were tested. Results showed that all four compounds showed great inhibitory effects. The IC50, the inhibitor concentrations leading to 50% activity lost,were estimated to be 2.88, 0. 93, 3. 60 and 0. 22 μmol/L. This meant that these four compounds had the potential to use as pesticide designing based on PP. Meanwhile, this study provided data to further inhibitor design.

关 键 词：菜青虫 酚氧化酶 缩氨基硫脲 合成 抑制作用 

分 类 号：Q356.1[生物学—遗传学]