School of Materials Science and Engineering, South China University of Technology, 381 Wushan Rd., Guangzhou, 510641, Guangdong, China.
College of Materials and Energy, South China Agricultural University, 483 Wushan Rd., Guangzhou, 510642, Guangdong, China.
Fungal Biol. 2020 Aug;124(8):735-741. doi: 10.1016/j.funbio.2020.04.007. Epub 2020 May 26.
A series of linear hydrophilic cationic polymers with different charge density and molecular weights were synthesized by one-step polymerization process. The effect of the hydrophobicity and molecular weights on the antifungal activity against Rhizoctonia solani (R. solani) and Fusarium oxysporum f. sp. cubense race 4 (Foc4) was assessed. The biotoxicity of the cationic polymers were evaluated based on their median lethal concentration (LC) for zebrafish and silkworm and median lethal dose (LD) for Kunming mice. The results indicated that the balance between antifungal activity and biotoxicity could be well tuned by controlling the hydrophobic-hydrophilic balance. The minimum inhibitory concentration (MIC) of PEPB10 and PEPB25 against R. solani were 160 μg/mL and 80 μg/mL, respectively. And the LD for Kunming mice of PEPB10 and PEPB25 were more than 5000 mg/kg, which mean that PEPB10 and PEPB25 with high hydrophilicity show low toxicity and better selectivity for R. solani. The cationic polymers can kill the R. solani by damaging their membranes and exchanging the Ca or/and Mg cations of their membranes or cell wall. These results help to understand the antifungal mechanism of low-toxic polymeric quaternary ammonium salts and highlight their potential application as highly selective fungicidal agents for controlling plant diseases.
通过一步聚合反应合成了一系列具有不同电荷密度和分子量的线性亲水阳离子聚合物。评估了疏水性和分子量对防治丝核菌(R. solani)和尖孢镰刀菌古巴专化型 4 号(Foc4)的抗真菌活性的影响。根据阳离子聚合物对斑马鱼和家蚕的半数致死浓度(LC)和昆明小鼠的半数致死剂量(LD)评估了其生物毒性。结果表明,通过控制疏水性-亲水性平衡,可以很好地调节抗真菌活性和生物毒性之间的平衡。PEPB10 和 PEPB25 对 R. solani 的最小抑菌浓度(MIC)分别为 160 μg/mL 和 80 μg/mL。PEPB10 和 PEPB25 对昆明小鼠的 LD 均大于 5000 mg/kg,这意味着具有高亲水性的 PEPB10 和 PEPB25 表现出低毒性和对 R. solani 的更好选择性。阳离子聚合物可以通过破坏其细胞膜以及交换其细胞膜或细胞壁中的 Ca 或/和 Mg 阳离子来杀死 R. solani。这些结果有助于理解低毒聚合季铵盐的抗真菌机制,并突出其作为防治植物病害的高选择性杀菌剂的潜在应用。