School of Pharmacy, Lanzhou University, Lanzhou 730000, People's Republic of China.
State Key Laboratory of Herbage Improvement and Grassland Agro-Ecosystems, College of Pastoral Agriculture Science and Technology, Lanzhou University, Lanzhou 730000, China.
J Agric Food Chem. 2024 Apr 10;72(14):7716-7726. doi: 10.1021/acs.jafc.3c08858. Epub 2024 Mar 27.
The emergence of resistant pathogens has increased the demand for alternative fungicides. The use of natural products as chemical scaffolds is a potential method for developing fungicides. HWY-289, a semisynthetic protoberberine derivative, demonstrated broad-spectrum and potent activities against phytopathogenic fungi, particularly (with EC values of 1.34 μg/mL). SEM and TEM imaging indicated that HWY-289 altered the morphology of the mycelium and the internal structure of cells. Transcriptomics revealed that it could break down cellular walls through amino acid sugar and nucleotide sugar metabolism. In addition, it substantially decreased chitinase activity and chitin synthase gene () expression by 53.03 and 82.18% at 1.5 μg/mL, respectively. Moreover, this impacted the permeability and integrity of cell membranes. Finally, HWY-289 also hindered energy metabolism, resulting in a significant reduction of ATP content, ATPase activities, and key enzyme activities in the TCA cycle. Therefore, HWY-289 may be a potential candidate for the development of plant fungicides.
耐药病原体的出现增加了对替代杀菌剂的需求。利用天然产物作为化学支架是开发杀菌剂的一种潜在方法。HWY-289 是一种半合成原小檗碱衍生物,对植物病原真菌表现出广谱和强大的活性,特别是(EC 值为 1.34 μg/mL)。SEM 和 TEM 成像表明,HWY-289 改变了菌丝体的形态和细胞的内部结构。转录组学研究表明,它可以通过氨基酸糖和核苷酸糖代谢分解细胞壁。此外,它在 1.5 μg/mL 时分别使几丁质酶活性和几丁质合成酶基因 () 表达降低 53.03%和 82.18%。此外,这会影响细胞膜的通透性和完整性。最后,HWY-289 还阻碍了能量代谢,导致 ATP 含量、ATP 酶活性和三羧酸循环中的关键酶活性显著降低。因此,HWY-289 可能是开发植物杀菌剂的潜在候选物。