Key Laboratory of Pesticide and Chemical Biology of Ministry of Education, College of Chemistry, Central China Normal University, Wuhan, China.
Department of Molecular Biosciences and Bioengineering, University of Hawaii at Manoa, Honolulu, HI, USA.
Pest Manag Sci. 2024 Feb;80(2):414-425. doi: 10.1002/ps.7771. Epub 2023 Sep 26.
Crop diseases caused by plant pathogenic fungi and bacteria have led to substantial losses in global food production. Chemical pesticides have been widely used as a primary means to mitigate these issues. Nevertheless, the persistent and excessive use of pesticides has resulted in the emergence of microbial resistance. Moreover, the improper application and excessive utilization of pesticides can contribute to environmental pollution and the persistence of pesticide residues. Consequently, the development of novel and highly effective bactericides and fungicides to combat plant pathogens holds immense practical importance.
A series of uracil hydrazones IV-B was deliberately designed and evaluated for their antimicrobial efficacy. The results of bioassays indicated that most IV-B exhibited >80% inhibition against the fungal species Monilia fructigena and Sclerotium rolfsii, as well as the bacterial species Clavibacter michiganensis subsp. michiganensis, Xanthomonas oryzae pv. oryzae, and Ralstonia solanacearum, at 50 μg/mL in vitro. In vivo, IV-B20 showed 89.9% of curative and 71.8% of protective activities against C. michiganensis subsp. michiganensis at 100 μg/mL superior to thiodiazole copper and copper hydroxide. IV-B20 also showed excellent protective activity against M. fructigena (96.3% at 200 μg/mL) and S. rolfsii (80.4% at 1000 μg/mL), which were greater than chlorothalonil and equivalent to thifluzamide. Mechanistic studies revealed that IV-B20 induced oxidative damage in pathogenic bacteria and promoted the leakage of cellular contents.
This study suggests that IV-B20 with uracil hydrazone skeleton has great potential as an antimicrobial candidate. These findings lay a foundation for practical application in agriculture. © 2023 Society of Chemical Industry.
由植物病原真菌和细菌引起的作物病害导致了全球粮食生产的重大损失。化学农药已被广泛用作减轻这些问题的主要手段。然而，农药的持续和过度使用导致了微生物抗性的出现。此外，农药的不当使用和过度利用会导致环境污染和农药残留的持久性。因此，开发新型、高效的杀菌剂和杀真菌剂来防治植物病原体具有重要的实际意义。
我们精心设计并评估了一系列尿嘧啶腙 IV-B 对其抗菌功效的影响。生物测定结果表明，在体外，大多数 IV-B 对真菌物种 Monilia fructigena 和 Sclerotium rolfsii 以及细菌物种 Clavibacter michiganensis subsp. michiganensis、Xanthomonas oryzae pv. oryzae 和 Ralstonia solanacearum 在 50μg/mL 时表现出 >80%的抑制作用。在体内，IV-B20 在 100μg/mL 时对 C. michiganensis subsp. michiganensis 的治疗活性为 89.9%，保护活性为 71.8%，优于噻二唑铜和氢氧化铜。IV-B20 对 M. fructigena（在 200μg/mL 时为 96.3%）和 S. rolfsii（在 1000μg/mL 时为 80.4%）也表现出极好的保护活性，优于百菌清，与噻呋酰胺相当。机制研究表明，IV-B20 诱导病原细菌发生氧化损伤并促进细胞内容物泄漏。
本研究表明，具有尿嘧啶腙骨架的 IV-B20 具有作为抗菌候选物的巨大潜力。这些发现为在农业中的实际应用奠定了基础。© 2023 化学工业协会。
