Though antibiotics have been used for decades to treat bacterial infections, there is a great need for new treatment methods. Bacteria are becoming resistant to conventional antibiotics, as is the case with Methicillin resistant Staphylococcus aureus (MRSA). Herein we report the design of a series of lipidated α/Sulfono-α-AA heterogeneous peptides as mimics for Host Defense Peptides (HDPs). Utilizing fluorescence microscopy and depolarization techniques, our compounds demonstrate the ability to kill Gram-positive bacteria through cell membrane disruption. This mechanism of action makes it difficult for bacteria to develop resistance. Further time kill studies and hemolytic assays have also proven these compounds to be efficient in their ability to eradicate bacteria cells while remaining non-toxic to human red blood cells. This new class of peptidomimetics shows promise for the future antibiotic treatment of MRSA.

中文翻译：

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脂化 α/磺基-α-AA 异质肽作为 MRSA 的抗菌剂。

尽管几十年来一直使用抗生素来治疗细菌感染，但仍然非常需要新的治疗方法。细菌对传统抗生素产生耐药性，耐甲氧西林金黄色葡萄球菌 (MRSA) 就是这种情况。在此，我们报告了一系列脂质化 α/磺基-α-AA 异质肽的设计，作为宿主防御肽 (HDP) 的模拟物。利用荧光显微镜和去极化技术，我们的化合物证明能够通过破坏细胞膜杀死革兰氏阳性细菌。这种作用机制使得细菌很难产生耐药性。进一步的时间杀灭研究和溶血测定也证明这些化合物能够有效地消灭细菌细胞，同时对人类红细胞保持无毒。这种新型肽模拟物为未来 MRSA 的抗生素治疗带来了希望。