Beijing Advanced Innovation Center for Food Nutrition and Human Health, National Center for Veterinary Drug Safety Evaluation, College of Veterinary Medicine, China Agricultural University, Yuanmingyuan West Road No.2, Beijing, 100193, China.
Institute of Food Safety, Department of Veterinary Sciences, Ludwig-Maximilians-University Munich, 85764, Oberschleißheim, Germany.
Angew Chem Int Ed Engl. 2017 Feb 1;56(6):1486-1490. doi: 10.1002/anie.201609277. Epub 2017 Jan 11.
The emergence and rapid spread of methicillin-resistant Staphylococcus aureus (MRSA) poses a serious threat to public health. New antibiotics and strategies are urgently needed to combat S. aureus associated infections. Bacaucin, a novel cyclic lipopeptide from Bacillus subtilis CAU21, is reported. Bacaucin shows broad antibacterial activity against Gram-positive bacteria, but is also hemolytic and cytotoxic. However, bacaucin-1, a bacaucin-inspired ring-opened heptapeptide, shows specific antibacterial activity against MRSA by a membrane-disruptive mechanism without detectable toxicity to mammalian cells or induction of bacterial resistance. Bacaucin-1 was efficient in preventing infections in both in vitro and in vivo models and is a valuable prototype antibiotic with high potential against S. aureus infections.
耐甲氧西林金黄色葡萄球菌 (MRSA) 的出现和迅速传播对公共健康构成了严重威胁。急需新的抗生素和策略来对抗金黄色葡萄球菌相关感染。枯草芽孢杆菌 CAU21 产生的新型环状脂肽 Bacaucin 具有报道。Bacaucin 对革兰氏阳性菌具有广泛的抗菌活性，但也具有溶血和细胞毒性。然而，Bacaucin-1 是一种受 Bacaucin 启发的开环七肽，通过破坏细胞膜的机制对 MRSA 具有特异性抗菌活性，对哺乳动物细胞没有检测到毒性，也不会诱导细菌耐药性。Bacaucin-1 在体外和体内模型中都能有效预防感染，是一种具有高潜力的抗金黄色葡萄球菌感染的有价值原型抗生素。
