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Temporin-GHb-DerivednPeptides Exhibit Potent Antibacterialnand Antibiofilm Activities against Staphylococcus aureus In Vitro and Protect Mice from Acute Infectious Pneumonia temporin - ghb衍生的肽显示出对金黄色葡萄球菌的有效抗菌和抗生物膜活性，并保护小鼠免受急性感染性肺炎

Figshare Pub Date : 2023-03-02 DOI: 10.1021/acsinfecdis.2c00544.s001

Xiao Jin (476848), Xuanyu Hu (13966818), Shangjun Jiang (4452043), Ting Zhao (434093), Yanmei Zha (14708972), Shuangshuang Wei (2571175), Jianguo Zhao (692807), Manchuriga Wang (5669108), Yingxia Zhang (5669114)

{"title":"Temporin-GHb-DerivednPeptides Exhibit Potent Antibacterialnand Antibiofilm Activities against Staphylococcus aureus In Vitro and Protect Mice from Acute Infectious Pneumonia","authors":"Xiao Jin (476848), Xuanyu Hu (13966818), Shangjun Jiang (4452043), Ting Zhao (434093), Yanmei Zha (14708972), Shuangshuang Wei (2571175), Jianguo Zhao (692807), Manchuriga Wang (5669108), Yingxia Zhang (5669114)","doi":"10.1021/acsinfecdis.2c00544.s001","DOIUrl":"https://doi.org/10.1021/acsinfecdis.2c00544.s001","url":null,"abstract":"With the continuous development of drug resistance innbacterianto traditional antibiotics, the demand for novel antibacterial agentsnis urgent. Antimicrobial peptides (AMPs) are promising candidatesnbecause of their unique mechanism of action and low tendency to inducendrug resistance. Previously, we cloned temporin-GHb (hereafter referrednto simply as “GHb”) from Hylarana guentheri. In this study, a series of derived peptides were designed, namely,nGHbR, GHbK, GHb3K, GHb11K, and GHbK4R. The five derived peptides hadnstronger antibacterial activities against Staphylococcus aureus than the parent peptide GHb and could effectively inhibit the formationnof biofilms and eradicate mature biofilms in vitro. GHbR, GHbK, GHb3K,nand GHbK4R exerted bactericidal effects by disrupting membrane integrity.nHowever, GHb11K exhibited bacteriostatic efficacy with toroidal porenformation on the cell membrane. In comparison to GHbK4R, GHb3K showednmuch lower cytotoxicity against A549 alveolar epithelial cells, withnan IC50 > 200 μM, which was much higher than itsnminimal inhibitory concentration (MIC = 3.1 μM) against S. aureus. The anti-infection potential of GHbK4R and GHb3Knwas investigated in vivo. Compared with vancomycin, the two peptidesndisplayed significant efficacy in a mouse model of acute pneumonianinfected with S. aureus. Both GHbK4R and GHb3K alsonhad no obvious toxicity to normal mice after intraperitoneal administrationn(15 mg/kg) for 8 days. Our results indicate that GHb3K and GHbK4Rnmight be promising candidates for the treatment of bacterial pneumonianinfected with S. aureus.","PeriodicalId":522590,"journal":{"name":"Figshare","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147899787","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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