纳米三臂星形聚合物的设计合成及负载氟啶胺性能研究

    Design and synthesis of a nanometric three-armed star-shaped polymer compound and study on the performance of fluazinam-loaded

    • 摘要: 本研究设计合成了纳米三臂星形聚合物 (TaSPC) 载药新材料,并用其负载疏水性广谱杀菌剂氟啶胺,制备了TaSPC/氟啶胺纳米载药颗粒。通过分子对接模拟及紫外分光光度法,探究了TaSPC负载氟啶胺的原理及载药性能;通过透射电镜与扫描电镜观察,对比分析了TaSPC负载氟啶胺前后的外观形貌及粒径变化;通过Zeta电位分析、与草莓叶片的接触角测定及罗丹明6G荧光标记TaSPC的内吸性测试,表征了TaSPC及TaSPC/氟啶胺的理化性质。通过室内离体及活体试验,测定了TaSPC/氟啶胺对4种植物病原真菌的抑菌效果、TaSPC对人体脐静脉内皮细胞的毒性以及TaSPC和TaSPC/氟啶胺对意大利蜜蜂的毒性。结果表明:TaSPC可通过疏水作用自发地与氟啶胺结合,农药负载率 (PLC) 为9%;TaSPC/氟啶胺粒径为17.86 nm,比氟啶胺原药的62.46 nm显著下降了71.4%;采用TaSPC负载后,TaSPC/氟啶胺液滴在草莓叶片上的接触角由氟啶胺原药的44.08° 降至33.60°,降低了23.78%。TaSPC/氟啶胺对植物病原真菌的抑制效果比氟啶胺原药显著提高,其中对草莓灰霉病菌(Botrytis cinerea)的抑制活性最高,0.2 mg/L剂量下,TaSPC/氟啶胺的抑制率达到75%,比氟啶胺原药提高近60%。在合理应用范围内,TaSPC 具有较低的细胞毒性,且TaSPC和TaSPC/氟啶胺对授粉蜜蜂的毒性也较低。研究表明,TaSPC对高效低毒纳米载体材料的开发及减少农药用量等方面均具有重要参考意义。

       

      Abstract: This study designed and synthesized a new drug-loading nanomaterial, the three-armed star-shaped polymer compound (TaSPC), and loaded the broad-spectrum fungicide fluazinam to prepare TaSPC/fluazinam nanocarrier particles. The principle and drug-loading performance of TaSPC loading fluazinam were investigated by molecular docking simulation and ultraviolet spectrophotometry. The appearance and particle size changes before and after loading fluazinam onto TaSPC were compared and analyzed by transmission electron microscopy and scanning electron microscopy. The physicochemical properties of TaSPC and TaSPC/fluazinam were characterized by Zeta potential analysis, contact angle measurement with strawberry leaves, and uptake test with Rhodamine 6G. The in vitro and in vivo inhibitory effects of TaSPC/fluazinam on four plant pathogenic fungi, the toxicity of TaSPC to human umbilical vein endothelial cells, and the toxicity of TaSPC and TaSPC/fluazinam to Apis mellifera ligustica Spin. were determined. The results indicated that TaSPC could spontaneously combine with fluazinam through hydrophobic interaction, with a pesticide loading rate (PLC) of 9%. The particle size of TaSPC/fluazinam was 17.86 nm, which was significantly reduced by 71.4% compared to the original fluazinam (62.46 nm). After loading with TaSPC, the contact angle of the TaSPC/fluazinam droplet on strawberry leaves decreased from 44.08° to 33.60°, a significant reduction of 23.78%. The inhibitory effect of TaSPC/fluazinam on plant pathogenic fungi was significantly enhanced compared to the original fluazinam. Among them, the inhibitory activity against Botrytis cinerea was the highest, with an inhibition rate of 75% at a dose of 0.2 mg/L, an increase of nearly 60% compared to the original fluazinam. Within a reasonable application range, TaSPC had low cytotoxicity, and both TaSPC and TaSPC/fluazinam had low toxicity to pollinating bees. The study demonstrated that TaSPC is a significant benchmark for the development of efficient and low-toxicity nanocarrier materials and the reduction of pesticide use.

       

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