以昆虫鱼尼丁受体为靶标的化合物活性筛选方法研究进展

昆虫鱼尼丁受体(ryanodine receptor,RyR)是目前新型杀虫剂创制中备受关注的靶标之一。在以RyR为靶标的杀虫剂氟虫酰胺和氯虫酰胺商品化后,大量基于该靶标的新型化合物被设计并合成出来。为加速研发和快速准确筛选以昆虫RyR为靶标的药剂,主要以氟虫酰胺和氯虫酰胺的活性筛选研究为例,对作用于RyR化合物的各种活体筛选方法和离体筛选方法进行了综述。其中活体筛选方法主要包括:点滴法、浸叶法、浸卵法、浸虫法、注射法和喷雾法;离体筛选方法主要包括MTT法、膜片钳技术、荧光技术、膜片钳技术与荧光技术结合以及计算机模拟筛选。通过对各种方法的分析比较,认为离体筛选方法快速、准确,在新型RyR杀虫剂活性的筛选研究中将进一步得到应用。

Progress on biological screening method for ryanodine receptor-targeted compounds

Insect ryanodine receptor (RyR) is becoming one of the most concerned targets for the development of novel insecticides.Since flubendiamide and chlorantraniliprole,RyR activators,were developed,many new compounds have been designed and synthesized on the basis of RyR structure.To develop and screen the compounds targeting at RyR acceleratedly and accurately,the biological screening methods for ryanodine receptor-targeted compounds were reviewed,taking the biological screening of flubendiamide and chlorantraniliprole for example.And six screening methods in vivo were included, such as topical application bioassay, leaf dipping method, eggs dipping method,immersion of the insect body,injection method and spraying method;and screening methods in vitro include MTT assay,patch clamp technology,fluorescence technology,patch clamp-fluorescence combination technology,and virtual screening.Quick and accurate screening method in vitro would be further used in the biological screening for novel RyR insecticides by comparing the advantages and disadvantages of these methods.