Nano-Sized Lipidated Dendrimers as Potent and Broad-Spectrum Antibacterial Agents
Nano-Sized Lipidated Dendrimers as Potent and Broad-Spectrum Antibacterial Agents
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DOI：
10.1002/marc.201800622
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发表时间：
2018-12-01
影响因子：
4.6
通讯作者：
Cai, Jianfeng
中科院分区：
文献类型：
--
作者：
Gide, Mussie;Nimmagadda, Alekhya;Cai, Jianfeng
由于与宿主防御肽（HDPs）相比易于合成和低制造成本，对开发包括树枝状聚合物的抗微生物聚合物有相当大的兴趣。在此，提出了一类新的纳米材料-脂化两亲性树枝状聚合物，其通过损害细菌细胞膜来模拟HDPs的抗菌机制。不同于传统的树枝状聚合物，制备一代一代对称的分子量分布，这些脂质化的树枝状聚合物上制备的固相与悬挂的脂质尾巴和精确控制的结构。通过合理的设计表明，这些脂化树枝状聚合物对革兰氏阳性和革兰氏阴性细菌，包括多重耐药菌株显示出有效的和选择性的抗微生物活性。除了对嗜热菌的抗菌活性外，这些树枝状聚合物还显示出有效抑制细菌生物膜。这类树枝状大分子作为一类新的生物材料，可能会导致一个有用的一代抗生素药物的实际应用。
There is considerable interest in the development of antimicrobial polymers including dendrimers due to the ease of synthesis and low manufacturing cost compared to host defense peptides (HDPs). Herein, a new class of nanomaterials-lipidated amphiphilic dendrimers-is presented that mimic the antibacterial mechanism of HDPs by compromising bacterial cell membranes. Unlike conventional dendrimers that are prepared generation by generation symmetrically with molecular weight distribution, these lipidated dendrimers are prepared on the solid phase with a hanging lipid tail and precisely controlled structure. It is shown through rational design that these lipidated dendrimers display potent and selective antimicrobial activity against both Gram-positive and Gram-negative bacteria, including multidrug-resistant strains. In addition to antibacterial activity against planktonic bacteria, these dendrimers are also shown to inhibit bacterial biofilms effectively. This class of dendrimers as a new class of biomaterials may lead to a useful generation of antibiotic agents with practical applications.