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新型自组装抗菌肽CR-16的性质及抑菌活性研究OACSTPCD

Properties and antibacterial activity of novel self-assembled antibacterial peptide CR-16

中文摘要英文摘要

目的 研究新型自组装多肽CR-16的性质及其对于大肠杆菌的抑菌活性,为细菌感染的治疗提供实验依据.方法 在抗菌肽Buforin Ⅱ和LfcinB结构基础上,设计并合成了新型抗菌肽CR-16,采用粒径、电位、透射电镜、X线衍射仪等手段表征该抗菌肽的性质.在测定临界胶束浓度的基础上,采用原子力显微镜、圆二色谱法等对分子的自组装性能进行考察.采用二倍稀释法测定该肽的最小抑菌浓度,并运用透射电子显微镜分析其对细菌外膜的影响.结果 抗菌肽CR-16能够成功自组装,自组装体呈现规则圆球状,性质稳定.抑菌实验表明,CR-16对3种大肠杆菌的生长均有抑制作用.值得重视的是,CR-16对产新德里金属-β-内酰胺酶1(NDM-1)的耐碳青霉烯类大肠杆菌生长有明显抑制作用,显示了其在抗细菌感染及抗耐药菌感染中的良好前景.结论 CR-16抗菌肽可以实现自组装,并且对大肠杆菌具有抑菌活性.

Objective To study the properties and antimicrobial activity of the novel self-assembled antimicrobial peptide(AMP)CR-16,and to provide experimental evidence for the treatment of bacterial infections.Methods CR-16 was designed and synthesized based on the structure of antimicrobial peptides Buforin Ⅱ and LfcinB.Dynamic light scattering(DLS),transmission electron microscopy(TEM),and X-ray diffraction(XRD)were used to characterize CR-16.Based on the results of critical micelle concentration(CMC),the self-assembled properties of CR-16 were investigated using atomic force microscopy(AFM)and circular dichroism(CD).The minimum inhibitory concentration(MIC)was used to study the inhibitory effect of CR-16 while transmission electron microscopy(TEM)was adopted to observe the interactions between CR-16 and the outer membrane of bacteria.Results AMP CR-16 was prepared as self-assemblies,which were regularly spherical in shape and stable in activity.CR-16 could inhibit both the growth of Escherichia coli and,more importantly,the growth of NDM-1-producing carbapenem-resistant Escherichia coli,promising good prospects in treating infections caused by antibiotic-resistant bacteria.Conclusion CR-16 can be self-assembled and deliver antibacterial effects against Escherichia coli.

崔亚楠;邹鹏飞;龚伟;王玉丽;高春生;杨阳;杨美燕

军事科学院军事医学研究院,北京 100850

药学

抗菌肽自组装抗生素耐药大肠杆菌抑菌活性

antimicrobial peptidesself-assemblyantibiotic resistanceEscherichia coliantimicrobial activity

《军事医学》 2024 (005)

369-375 / 7

10.7644/j.issn.1674-9960.2024.05.008

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