PDF(Pubmed)
Abstract：
The research on new compounds against plant pathogens is still socially and economically important. It results from the increasing resistance of pests to plant protection products and the need to maintain high yields of crops, particularly oilseed crops used to manufacture edible and industrial oils and biofuels. We tested thirty-five semi-synthetic hydrazide-hydrazones with aromatic fragments of natural origin against phytopathogenic laccase-producing fungi such as Botrytis cinerea, Sclerotinia sclerotiorum, and Cerrena unicolor. Among the investigated molecules previously identified as potent laccase inhibitors were also strong antifungal agents against the fungal species tested. The highest antifungal activity showed derivatives of 4-hydroxybenzoic acid and salicylic aldehydes with 3-tert-butyl, phenyl, or isopropyl substituents. S. sclerotiorum appeared to be the most susceptible to the tested compounds, with the lowest IC50 values between 0.5 and 1.8 µg/mL. We applied two variants of phytotoxicity tests for representative crop seeds and selected hydrazide-hydrazones. Most tested molecules show no or low phytotoxic effect for flax and sunflower seeds. Moreover, a positive impact on seed germination infected with fungi was observed. With the potential for application, the cytotoxicity of the hydrazide-hydrazones of choice toward MCF-10A and BALB/3T3 cell lines was lower than that of the azoxystrobin fungicide tested.
摘要：
针对植物病原体的新化合物的研究仍然具有社会和经济意义。这是由于害虫对植物保护产品的抵抗力不断增强以及需要保持作物的高产量，特别是用于制造食用和工业油和生物燃料的油料作物。我们测试了35种半合成酰肼-腙与天然来源的芳香片段对抗植物病原漆酶产生真菌，如灰霉病菌，菌核病,还有Cerrenaunicolor.在先前鉴定为有效漆酶抑制剂的研究分子中,也是针对所测试真菌物种的强抗真菌剂。最高的抗真菌活性显示4-羟基苯甲酸和水杨醛与3-叔丁基的衍生物，苯基,或异丙基取代基。菌核病菌似乎对测试化合物最敏感，最低IC50值在0.5至1.8µg/mL之间。我们对代表性作物种子和选定的酰肼-腙应用了两种植物毒性测试变体。大多数测试的分子对亚麻和向日葵种子没有或显示低的植物毒性作用。此外，观察到真菌感染对种子萌发的积极影响。随着应用的潜力，选择的酰肼-腙对MCF-10A和BALB/3T3细胞系的细胞毒性低于测试的唑菌酯杀真菌剂。
