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First Anti-ToCV Activity Evaluation of Glucopyranoside Derivatives Containing a Dithioacetal Moiety through a Novel ToCVCP-Oriented Screening Method
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2019-04-26 00:00:00 , DOI: 10.1021/acs.jafc.9b01265
Dandan Xie 1 , Jian Zhang 1 , Huanyu Yang 1 , Yuewen Liu 1 , Deyu Hu 1 , Baoan Song 1
Affiliation  

Tomato chlorosis virus (ToCV) is a newly reported plant virus that has rapidly spread to all parts of the world, resulting in a serious decline in tomato quality and yield due to the lack of effective control agents. In this study, the ToCV coat protein (ToCVCP) was expressed and purified in Escherichia coli, and a series of novel glucopyranoside derivatives containing a dithioacetal moiety was designed and synthesized. The binding affinity of these compounds to ToCVCP was determined using microscale thermophoresis. Results revealed that compounds 6b and 8a interacted with ToCVCP with Kd values of 0.12 and 0.21 μM, respectively. Quantitative reverse transcription polymerase chain reaction was used to evaluate the anti-ToCV activity of 6b and 8a in vivo, and both significantly reduced the expression level of ToCVCP gene in tomato compared with commercial antivirus agents. This study provides an efficient and convenient screening method for anti-ToCV agents and reliable support for the development of novel agrochemicals for ToCV.

中文翻译:

通过一种新型的面向ToCVCP的筛选方法,首次对含二硫缩醛基的葡糖苷衍生物的抗ToCV活性进行评估

番茄绿化病毒(ToCV)是一种新近报道的植物病毒,已迅速传播到世界各地,由于缺乏有效的控制剂,导致番茄质量和单产严重下降。在这项研究中,ToCV外壳蛋白(ToCVCP)在大肠杆菌中表达和纯化,并设计和合成了一系列含有二硫缩醛部分的新型吡喃葡萄糖苷衍生物。这些化合物对ToCVCP的结合亲和力是使用微尺度热泳法测定的。结果表明,化合物6b8a与ToCVCP相互作用,K d值分别为0.12和0.21μM。定量逆转录聚合酶链反应用于评估6b8a在体内的抗ToCV活性,与市售抗病毒剂相比,两者均显着降低了ToCVCP基因在番茄中的表达水平。这项研究为抗ToCV药剂提供了一种高效便捷的筛选方法,并为开发新型ToCV农药提供了可靠的支持。
更新日期:2019-04-26
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