School of Pharmacy, Lanzhou University, Lanzhou 730000, People's Republic of China.
School of Pharmacy, Southwest Minzu University, Chengdu 610041, China.
J Agric Food Chem. 2024 Sep 25;72(38):20882-20891. doi: 10.1021/acs.jafc.4c05968. Epub 2024 Sep 11.
Naturally derived compounds show promise as treatments for microbial infections. Polyphenols, abundantly found in various plants, fruits, and vegetables, are noted for their physiological benefits including antimicrobial effects. This study introduced a new set of acylated phloroglucinol derivatives, synthesized and tested for their antifungal activity in vitro against seven different pathogenic fungi. The standout compound, 3-methyl-1-(2,4,6-trihydroxyphenyl) butan-1-one (), exhibited remarkable fungicidal strength, with EC values of 1.39 μg/mL against and 1.18 μg/mL against , outperforming previously screened phenolic compounds. When tested in vivo, demonstrated effective antifungal properties, with cure rates of 76.26% for brown rot and 83.35% for gray mold at a concentration of 200 μg/mL, rivaling the commercial fungicide Pyrimethanil in its efficacy against . Preliminary research suggests that s antifungal mechanism may involve the disruption of spore germination, damage to the fungal cell membrane, and leakage of cellular contents. These results indicate that compound has excellent fungicidal properties against and holds potential as a treatment for gray mold.
天然化合物显示出作为微生物感染治疗方法的潜力。多酚广泛存在于各种植物、水果和蔬菜中，以其生理益处而闻名，包括抗菌作用。本研究引入了一组新的酰化间苯三酚衍生物，合成并测试了它们对七种不同致病真菌的体外抗真菌活性。表现突出的化合物 3-甲基-1-(2,4,6-三羟基苯基)丁-1-酮 ()，表现出显著的杀菌强度，对 和 的 EC 值分别为 1.39 μg/mL 和 1.18 μg/mL，优于之前筛选的酚类化合物。在体内测试时，在 200 μg/mL 的浓度下，对褐腐病的治愈率为 76.26%，对灰霉病的治愈率为 83.35%，其疗效可与商业杀菌剂嘧啶菌胺媲美。初步研究表明，化合物 的抗真菌机制可能涉及孢子萌发的破坏、真菌细胞膜的损伤和细胞内容物的泄漏。这些结果表明，化合物 对 具有优异的杀菌性能，有望成为灰霉病的治疗方法。
