具有广泛的抗真菌活性的α,β-不和脂肪酸化物:设计,生物活性和作用机制
Tengyi Du1, Ruofei Bai1, Yiwei Wang1
1College of Chemistry & Pharmacy, Northwest A&F University, Yangling, Xianyang, Shaanxi 712100, People's Republic of China.
Journal of agricultural and food chemistry
|September 17, 2025
概括
新的不和脂肪酸N-烯化衍生物对植物病原体表现出强大的抗真菌活性. 化合物5s是一种强大的糖酸脱酶 (SDH) 抑制剂,表现出卓越的疗效和安全性,为农业杀菌剂提供了一个有希望的新头.
科学领域:
- 农业化学 农业化学
- 菌类学 菌类学是指菌类学.
- 有机合成 有机合成
背景情况:
- 化衍生物正在探索其抗真菌性质.
- 植物病原菌在全球范围内造成重大作物损失.
- 新型,有效和安全的杀菌剂的开发对于可持续农业至关重要.
研究的目的:
- 设计和合成阿尔法,β不和脂肪酸的新型N'-烯化衍生物.
- 为了评估它们在体外抗真菌活性对关键的植物病原菌.
- 阐明作用机制并评估有前途的候选人的安全概况.
主要方法:
- 合成N'-烯化衍生物.
- 在体外抗真菌测定对A. solani,A. brassicae,A. alternate,C. gloeosporioides和P. oryzae.进行检测.
- 使用电子显微镜,ROS检测,MMP评估和酶抑制试验 (SDH活性) 的机制研究.
- 分子对接和结构-活性关系 (SAR) 分析.
- 细胞毒性和植物毒性评估.
主要成果:
- 大多数合成的化合物表现出极好的抗真菌活性,EC50值在0.76-5.79μg/mL之间.
- 特定衍生品 (5a,5g,5s,5w) 与商用杀菌剂克雷索西姆-甲基相比显示出更高的疗效 (EC50:0.76-0.87μg/mL).
- 化合物5s在20μg/mL时完全抑制了真菌生长,对抗番茄果感染的效果与博斯卡利德相当,并且没有显著的植物毒性或细胞毒性.
- 机制研究揭示了菌根干扰,细胞膜损伤,ROS增加,MMP改变,和酸脱酶 (SDH) 活动的强烈抑制 (IC50 = 3.54μg/mL).
- 分子对接表明了4-基对SDH结合的重要性,SAR强调了4-素替代对抗真菌活性的好处.
结论:
- 阿尔法,贝塔不和脂肪酸的N'-基化物代表了一种新型的强效抗真菌剂.
- 化合物5s是一种高效和安全的候选物,通过SDH抑制和细胞损伤起作用.
- 这些发现支持这些化合物的发展成为有前途的农业杀菌剂.
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