Nanomedicine (Lond). 2015 Nov;10(22):3359-71. doi: 10.2217/nnm.15.137.
To explore the potential of de novo designed cyclic lipopeptides and its linear counterparts as antibacterial agents.
MATERIALS & METHODS: The lipopeptides were synthesized via solid-phase peptide synthesis and the cyclization was achieved by using succinic acid linker. The antimicrobial activities of the lipopeptides were evaluated in vitro against a variety selection of Gram-negative and Gram-positive bacteria including clinical isolates of multidrug-resistant strains.
The synthesized lipopeptides were able to self-assemble into nanoparticles in an aqueous environment, with three exhibiting potent antibacterial activity against Gram-positive bacteria, including clinically relevant multidrug-resistant bacteria.
The lead compounds have the potential to be developed as new antibacterials that are effective against Gram-positive bacteria, including multidrug-resistant isolates.
探索从头设计的环状脂肽及其线性类似物作为抗菌剂的潜力。
通过固相肽合成合成脂肽，并通过琥珀酸连接子实现环化。在体外评估脂肽对各种革兰氏阴性和革兰氏阳性细菌的抗菌活性，包括临床分离的多药耐药菌株。
合成的脂肽能够在水相环境中自组装成纳米颗粒，其中三种对革兰氏阳性菌，包括临床相关的多药耐药菌，具有很强的抗菌活性。
这些先导化合物有可能被开发成新的抗菌药物，对革兰氏阳性菌，包括多药耐药株具有疗效。
