Department of Chemistry, University of South Florida, 4202 E. Fowler Ave., Tampa, FL 33620, USA.
Department of Molecular Medicine, Morsani College of Medicine, University of South Florida, 12901 Bruce B Downs Blvd., Tampa, FL 33612, USA.
Int J Mol Sci. 2023 Mar 29;24(7):6407. doi: 10.3390/ijms24076407.
Antibiotic resistance is one of the most significant issues encountered in global health. There is an urgent demand for the development of a new generation of antibiotic agents combating the emergence of drug resistance. In this article, we reported the design of lipidated dendrimeric γ-AApeptides as a new class of antimicrobial agents. These AApeptides showed excellent potency and broad-spectrum activity against both Gram-positive bacteria and Gram-negative bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). The mechanistic studies revealed that the dendrimeric AApeptides could kill bacteria rapidly through the permeabilization of bacterial membranes, analogous to host-defense peptides (HDPs). These dendrimers also did not induce antibiotic resistance readily. The easy access to the synthesis, together with their potent and broad-spectrum activity, make these lipidated dendrimeric γ-AApeptides a new generation of antibacterial agents.
抗生素耐药性是全球健康面临的最重大问题之一。迫切需要开发新一代抗生素来对抗耐药性的出现。在本文中，我们报道了作为一类新型抗菌剂的脂质化树枝状γ-AApeptides 的设计。这些 AApeptides 对革兰氏阳性菌和革兰氏阴性菌均显示出优异的效力和广谱活性，包括耐甲氧西林金黄色葡萄球菌 (MRSA)。机制研究表明，树枝状 AApeptides 可以通过细菌膜的通透性迅速杀死细菌，类似于宿主防御肽 (HDP)。这些树枝状聚合物也不容易诱导抗生素耐药性。它们的合成方法简单，且具有强大的广谱活性，使这些脂质化树枝状 γ-AApeptides 成为新一代抗菌剂。
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