Modification of narrow‐spectrum peptidomimetic polyurethanes with fatty acid chains confers broad‐spectrum antibacterial activity
Modification of narrow‐spectrum peptidomimetic polyurethanes with fatty acid chains confers broad‐spectrum antibacterial activity
复制标题
用脂肪酸链修饰窄谱拟肽聚氨酯可赋予广谱抗菌活性
DOI：
10.1002/pi.5773
复制
发表时间：
2019
影响因子：
3.2
通讯作者：
Joy, Abraham
中科院分区：
文献类型：
--
作者：
Peng, Chao;Zhang, Tian;Ortiz‐Ortiz, Deliris N.;Vishwakarma, Apoorva;Barton, Hazel A.;Joy, Abraham
每年，成千上万的患者死于对传统抗生素治疗无效的耐药细菌感染。抗菌聚合物是对抗抗生素耐药细菌感染的一种有前途的新方法。我们之前报道了一系列窄谱拟肽抗菌聚氨酯的合成，这些聚氨酯可有效对抗革兰氏阴性菌，如大肠杆菌；然而，这些聚合物对革兰氏阳性细菌（例如金黄色葡萄球菌）无效。为了了解化学结构和抗菌活性之间的相关性，我们随后使用癸酸和油酸进行后聚合改性，开发了这些抗菌聚氨酯的三种结构变体。我们的结果表明，这种修饰将这些聚合物的窄谱抗菌活性转化为针对革兰氏阳性菌（如链球菌）的广谱活性。然而，金黄色葡萄球菌也增加了它们对哺乳动物细胞的毒性。细菌膜破坏的机制研究说明了各种聚合物之间抗菌作用的差异。结果证明了在抗菌聚合物组合物的设计中平衡抗菌活性和哺乳动物细胞相容性的挑战。 © 2019 中国化学工业学会
Each year, thousands of patients die from antimicrobial‐resistant bacterial infections that fail to respond to conventional antibiotic treatment. Antimicrobial polymers are a promising new method of combating antibiotic‐resistant bacterial infections. We have previously reported the synthesis of a series of narrow‐spectrum peptidomimetic antimicrobial polyurethanes that are effective against Gram‐negative bacteria, such asEscherichia coli; however, these polymers are not effective against Gram‐positive bacteria, such asStaphylococcus aureus. With the aim of understanding the correlation between chemical structure and antibacterial activity, we have subsequently developed three structural variants of these antimicrobial polyurethanes using post‐polymerization modification with decanoic acid and oleic acid. Our results show that such modifications converted the narrow‐spectrum antibacterial activity of these polymers into broad‐spectrum activity against Gram‐positive species such asS. aureus, however, also increasing their toxicity to mammalian cells. Mechanistic studies of bacterial membrane disruption illustrate the differences in antibacterial action between the various polymers. The results demonstrate the challenge of balancing antimicrobial activity and mammalian cell compatibility in the design of antimicrobial polymer compositions. © 2019 Society of Chemical Industry
含三唑环丁烯的开环复分解聚合：二嵌段共聚物的合成以及侧基大小对聚合动力学影响的评估
DOI：
--
发表时间：
2017
期刊：
影响因子：
--
作者：
Jia Wei;William S Trout;Y. C. Simon;S. Granados
通讯作者：
S. Granados