Chun Zhang, Kunhong Zhao, Zilin Wu, Na Tao, Weijia Yang, Zhaojia Li, Moxian Chen* and Xiangyang Li*,
{"title":"5-氟吲哚抑制拟靶蛋氨酸合成酶和丁香假单胞菌。actinidiae毒性","authors":"Chun Zhang, Kunhong Zhao, Zilin Wu, Na Tao, Weijia Yang, Zhaojia Li, Moxian Chen* and Xiangyang Li*, ","doi":"10.1021/acs.jafc.5c03647","DOIUrl":null,"url":null,"abstract":"<p >Bacterial canker caused by <i>Pseudomonas syringae</i> pv. <i>actinidiae</i> (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<sub>50</sub>) of 15.34 μg/mL, demonstrating a higher efficacy than the positive control copper hydroxide (EC<sub>50</sub> = 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 <i>methionine synthase II</i> (<i>MetE</i>) 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<sup>693</sup> is a key binding site and that there is no specific binding between 5-fluoroindole and the Psa MetE<sup>D693A</sup> mutant. This study provides valuable insights for developing effective agents to control kiwifruit bacterial canker.</p>","PeriodicalId":41,"journal":{"name":"Journal of Agricultural and Food Chemistry","volume":"73 26","pages":"16193–16204"},"PeriodicalIF":6.2000,"publicationDate":"2025-06-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"5-Fluoroindole Inhibits Its Putative Target Methionine Synthase and Pseudomonas syringae pv. actinidiae Virulence\",\"authors\":\"Chun Zhang, Kunhong Zhao, Zilin Wu, Na Tao, Weijia Yang, Zhaojia Li, Moxian Chen* and Xiangyang Li*, \",\"doi\":\"10.1021/acs.jafc.5c03647\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p >Bacterial canker caused by <i>Pseudomonas syringae</i> pv. <i>actinidiae</i> (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<sub>50</sub>) of 15.34 μg/mL, demonstrating a higher efficacy than the positive control copper hydroxide (EC<sub>50</sub> = 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 <i>methionine synthase II</i> (<i>MetE</i>) 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<sup>693</sup> is a key binding site and that there is no specific binding between 5-fluoroindole and the Psa MetE<sup>D693A</sup> mutant. This study provides valuable insights for developing effective agents to control kiwifruit bacterial canker.</p>\",\"PeriodicalId\":41,\"journal\":{\"name\":\"Journal of Agricultural and Food Chemistry\",\"volume\":\"73 26\",\"pages\":\"16193–16204\"},\"PeriodicalIF\":6.2000,\"publicationDate\":\"2025-06-23\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Agricultural and Food Chemistry\",\"FirstCategoryId\":\"97\",\"ListUrlMain\":\"https://pubs.acs.org/doi/10.1021/acs.jafc.5c03647\",\"RegionNum\":1,\"RegionCategory\":\"农林科学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"AGRICULTURE, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Agricultural and Food Chemistry","FirstCategoryId":"97","ListUrlMain":"https://pubs.acs.org/doi/10.1021/acs.jafc.5c03647","RegionNum":1,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"AGRICULTURE, MULTIDISCIPLINARY","Score":null,"Total":0}
5-Fluoroindole Inhibits Its Putative Target Methionine Synthase and Pseudomonas syringae pv. actinidiae Virulence
Bacterial canker caused by Pseudomonas syringae pv. actinidiae (Psa) severely impacts global kiwifruit production. This study shows that 5-fluoroindole exerts significant bactericidal activity against Psa, with a half-maximal effective concentration (EC50) of 15.34 μg/mL, demonstrating a higher efficacy than the positive control copper hydroxide (EC50 = 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 methionine synthase II (MetE) 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 Asp693 is a key binding site and that there is no specific binding between 5-fluoroindole and the Psa MetED693A mutant. This study provides valuable insights for developing effective agents to control kiwifruit bacterial canker.
期刊介绍:
The Journal of Agricultural and Food Chemistry publishes high-quality, cutting edge original research representing complete studies and research advances dealing with the chemistry and biochemistry of agriculture and food. The Journal also encourages papers with chemistry and/or biochemistry as a major component combined with biological/sensory/nutritional/toxicological evaluation related to agriculture and/or food.