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智能 β-环糊精主导的螺旋超分子树枝状组装体提高了叶面亲和力和生物膜破坏能力,可有效治疗严重的细菌病。

Smart β-cyclodextrin-dominated helical supramolecular dendritic assemblies improve the foliar affinity and biofilm disruption for treating alarming bacterial diseases.

机构信息

State Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals of Guizhou University, Guiyang 550025, China.

State Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals of Guizhou University, Guiyang 550025, China.

出版信息

Carbohydr Polym. 2025 Jan 15;348(Pt A):122823. doi: 10.1016/j.carbpol.2024.122823. Epub 2024 Oct 9.

Abstract

Recent outbreaks of alarming bacterial diseases have significantly impacted global agricultural productivity. Conventional bactericides exhibit certain limitations in efficiently impeding biofilm formation and annihilating biofilm-dispersed pathogens, and often expose to high off-target movement during foliar spraying. Here, we produce an innovative helical dendrimer-like supramolecular material (PhA28@β-CD) assembled by a bioactive small-molecule 2-chlorophenylisopropanolamine (PhA28) and β-cyclodextrin (β-CD) through host-guest recognition principle. In this system, the advisable optimization by a macrocyclic oligosaccharide-β-CD significantly enhances the water-solubility, biocompatibility, and bioavailability of PhA28. At a low-dose of 6.8 μg/mL, PhA28@β-CD discloses an outstanding biofilm disruption rate of 82.4 %, notably exceeding that of PhA28 (60.6 %), which thereby reduces the biofilm-associated virulence. Meanwhile, the self-assembled PhA28@β-CD possesses superior wetting and dispersing properties on hydrophobic leaves, leading to effective foliar deposition and prolong retention of active components. In vivo studies reveal that PhA28@β-CD exhibits superior curative (66.0 %) and protective (72.6 %) activities against citrus canker at 200 μg/mL, markedly surpassing those of the existing bactericide thiodiazole‑copper (46.8 % and 52.2 %) and single PhA28. This material also has broad-spectrum control efficiency (53.0 % ~ 59.5 %) against rice bacterial blight. This research lays the groundwork for developing carbohydrate-optimized multifunctional dendrimer-like assemblies aimed at disrupting biofilms and improving sustained bioavailability to combat bacterial diseases.

摘要

最近爆发的一些令人震惊的细菌性疾病对全球农业生产力造成了重大影响。传统的杀菌剂在有效阻止生物膜形成和消灭生物膜分散的病原体方面存在一定的局限性,并且在叶片喷施时经常会暴露在高的非靶标运动中。在这里,我们通过主客体识别原理,由一种生物活性小分子 2-氯苯异丙醇胺(PhA28)和β-环糊精(β-CD)组装了一种创新的螺旋树枝状超分子材料(PhA28@β-CD)。在这个系统中,大环寡糖-β-CD 的合理优化显著提高了 PhA28 的水溶性、生物相容性和生物利用度。在 6.8μg/mL 的低剂量下,PhA28@β-CD 显示出 82.4%的出色的生物膜破坏率,明显超过 PhA28(60.6%),从而降低了生物膜相关的毒力。同时,自组装的 PhA28@β-CD 具有优异的润湿和分散疏水性叶片的性能,导致有效叶片沉积和活性成分的延长保留。体内研究表明,PhA28@β-CD 在 200μg/mL 时对柑橘溃疡病表现出优异的治疗(66.0%)和保护(72.6%)活性,明显优于现有杀菌剂噻二唑铜(46.8%和 52.2%)和单一的 PhA28。该材料对水稻细菌性条斑病也具有广谱的防治效率(53.0%~59.5%)。本研究为开发旨在破坏生物膜和提高持续生物利用度以防治细菌性疾病的优化碳水化合物多功能树枝状组装体奠定了基础。

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