Strobilurin类杀菌剂作用靶标的研究进展

Strobilurin类杀菌剂是在具有杀菌活性的天然β-甲氧基丙烯酸酯衍生物的基础上研发出来的,具有广谱、高效、安全的特点。主要以粘噻唑为例综述了该类杀菌剂作用靶标及作用位点的研究过程及最新进展。生化作用机理的研究明确了粘噻唑作用于线粒体呼吸链bc1复合物中的细胞色素b及铁硫蛋白,阻止了从细胞色素b到细胞色素c1的电子传递,从而抑制线粒体的呼吸作用;蛋白质晶体学研究明确了粘噻唑的作用位点(Qo位点)是通过氢键与铁硫蛋白及细胞色素b的残基结合的。其他strobilurin类杀菌剂和粘噻唑具有相同的靶标,但由于各化合物之间存在一定的结构差异,其具体作用位点亦有一定的差别。

Advance in Research of the Target of Action of Strobilurin Fungicides

The invention of strobilurin fungicides was inspired by a series of fungicidally active natural products—the derivatives of β-methoxyacrylate group. The outstanding character of strobilurin fungicides was broad-spectrum of activity, long duration of action, high activity at low rates of application, and outstanding environmental tolerability. The progress of research on the target and action site of the class of fungicide were reviewed with fungicide—myxothiazol as a main example. Studies on the action target of myxothiazol by biochemical assays revealed that it inhibited the mitochondrial respiration by binding at cytochrome b and iron sulfur protein, thus blocking the electron transport from cytochrome b to c1. The site of action of myxothiazol (Qo site) was achieved by studies on protein crystal structure and binding of myxothiazol was stabilized by two hydrogen bonds with residue of cytochrome b and iron sulfur protein. Almost all of the strobilurin fungicides had a common target as myxothiazol by binding to the Qo site of the bc1 complex. Maybe , there were slight variances in specific site of action due to the difference in structure between different strobilurin fungicides.