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Broad-spectrum antimicrobial supramolecular assemblies with distinctive size and shape

机译:具有独特尺寸和形状的广谱抗菌超分子组装体

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摘要

With the increased prevalence of antibiotic-resistant infections, there is an urgent need for innovative antimicrobial treatments. One such area being actively explored is the use of self-assembling cationic polymers. This relatively new class of materials was inspired by biologically pervasive cationic host defense peptides. The antimicrobial action of both the synthetic polymers and naturally occurring peptides is believed to be complemented by their three-dimensional structure. In an effort to evaluate shape effects on antimicrobial materials, triblock polymers were polymerized from an assembly directing terephthalamide-bisurea core. Simple changes to this core, such as the addition of a methylene spacer, served to direct self-assembly into distinct morphologies-spheres and rods. Computational modeling also demonstrated how subtle core changes could directly alter urea stacking motifs manifesting in unique multidirectional hydrogen-bond networks despite the vast majority of material consisting of poly(lactide) (interior block) and cationic polycarbonates (exterior block). Upon testing the spherical and rod-like morphologies for antimicrobial properties, it was found that both possessed broad-spectrum activity (Gram-negative and Gram-positive bacteria as well as fungi) with minimal hemolysis, although only the rod-like assemblies were effective against Candida albicans.
机译:随着抗生素抗性感染的流行增加,迫切需要创新的抗微生物治疗。积极探索的此类领域之一是自组装阳离子聚合物的使用。这种相对较新的材料类别是受到生物渗透性阳离子宿主防御肽的启发。合成聚合物和天然存在的肽的抗微生物作用被认为由它们的三维结构所补充。为了评估形状对抗菌材料的影响,三嵌段聚合物是由引导对苯二甲酰胺-双脲核心的组装体聚合而成的。对该核心进行简单的更改,例如添加亚甲基间隔基,即可将自组装定向为不同的形态-球形和杆状。计算模型还表明,尽管绝大多数材料由聚(丙交酯)(内部嵌段)和阳离子聚碳酸酯(外部嵌段)组成,但是细微的核心变化如何直接改变独特的多方向氢键网络中表现出的尿素堆积图案。通过测试球形和棒状形态的抗菌性能,发现它们都具有广谱活性(革兰氏阴性和革兰氏阳性细菌以及真菌),溶血作用极小,尽管只有棒状组件有效反对白色念珠菌。

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