Zhang Chun, Zhao Kunhong, Wu Zilin, Tao Na, Yang Weijia, Li Zhaojia, Chen Moxian, Li Xiangyang
State Key Laboratory of Green Pesticide, Center for R&D of Fine Chemicals, Guizhou University, Huaxi District, Guiyang 550025, China.
Ministry of Agriculture Key Laboratory for Crop Pest Monitoring and Green Control, Joint International Research Laboratory of Crop Molecular Breeding, College of Plant Protection, China Agricultural University, Beijing 100193, China.
J Agric Food Chem. 2025 Jul 2;73(26):16193-16204. doi: 10.1021/acs.jafc.5c03647. Epub 2025 Jun 23.
Bacterial canker caused by pv. (Psa) severely impacts global kiwifruit production. This study shows that 5-fluoroindole exerts significant bactericidal activity against Psa, with a half-maximal effective concentration (EC) of 15.34 μg/mL, demonstrating a higher efficacy than the positive control copper hydroxide (EC = 58.65 μg/mL). 5-Fluoroindole disrupts membrane integrity, induces oxygen species (ROS) accumulation, and triggers apoptosis in Psa. Transcriptome analysis reveals that 5-fluoroindole treatment increased the expression of the () gene by 6.28 fold compared with the expression of this gene in the control (CK) group. Microscale thermophoresis and isothermal titration calorimetry show that the dissociation constants of the binding of 5-fluoroindole to MetE protein are 0.33 and 8.55 μM, respectively. Molecular docking experiments indicate that Asp is a key binding site and that there is no specific binding between 5-fluoroindole and the Psa MetE mutant. This study provides valuable insights for developing effective agents to control kiwifruit bacterial canker.
由丁香假单胞菌猕猴桃致病变种（Psa）引起的细菌性溃疡病严重影响全球猕猴桃产量。本研究表明，5-氟吲哚对Psa具有显著的杀菌活性，半数有效浓度（EC50）为15.34μg/mL，显示出比阳性对照氢氧化铜（EC50 = 58.65μg/mL）更高的效力。5-氟吲哚破坏膜完整性，诱导活性氧（ROS）积累，并触发Psa细胞凋亡。转录组分析显示，与对照组（CK）相比，5-氟吲哚处理使MetE基因的表达增加了6.28倍。微量热泳动和等温滴定量热法表明，5-氟吲哚与MetE蛋白结合的解离常数分别为0.33和8.55μM。分子对接实验表明，天冬氨酸是关键结合位点，且5-氟吲哚与Psa MetE突变体之间不存在特异性结合。本研究为开发控制猕猴桃细菌性溃疡病的有效药剂提供了有价值的见解。
