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首页> 外文期刊>RSC Advances >Self assembly and hydrogelation of spermine functionalized aromatic peptidomimetics against planktonic and sessile methicillin resistant S. aureus
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Self assembly and hydrogelation of spermine functionalized aromatic peptidomimetics against planktonic and sessile methicillin resistant S. aureus

机译：对浮游生物和无术甲氧西米尔抗金黄色葡萄球菌的精华官能化芳香族肽肽的自组装和水凝。

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摘要

Peptide amphipathicity is a common characteristic of self assembling peptide nanomaterials and host defense cationic antimicrobial peptides. In the present work, we utilized amphipathicity of ultra short aromatic sequences with spermine as a cationic C-terminal tag for designing of antibacterial hydrogels against multidrug resistant bacteria. These designed peptidomimetics acquired single walled-nanofibres and nanotubes that formed hydrogels at higher concentrations between 0.5-1% w/v at physiological pH. In vitro antibacterial studies of the nanofibres exhibited potent activity (MIC: 14.2-227.2 mu g mL(-1)) against Gram positive and Gram negative bacterial strains including clinically relevant pathogens such as methicillin resistant S. aureus (MRSA) and S. epidermidis. Bactericidal kinetic and scanning electron microscopy of peptidomimetics treated MRSA confirms the membrane active mode of action. These analogues also displayed a strong antibiofilm activity at the MIC level and demonstrated reduced viability of mature MRSA by > 50% biofilms at 0.5-2% w/v hydrogels. Moreover, the nanofibres were neither cytotoxic nor hemolytic in nature. With selective modes of interaction of the designed nanostructure with bacteria these hydrogels could be potentially therapeutic against MRSA wound infections and also as implantable biomaterials.
机译：肽两亲性是自组装肽纳米材料和宿主防阳极抗菌肽的常见特征。在本作工作中，我们利用超短芳族序列的伴有精芳烃作为阳离子C末端标签，用于设计针对多药抗性细菌的抗菌水凝胶。这些设计的肽模拟物获取了在生理pH下在0.5-1％w / v之间形成的单壁纳米纤维和纳米管形成水凝胶。纳米纤维的体外抗菌研究表现出浓郁的活性（MIC：14.2-227.2μgmml（-1）），克革克阳性和革兰氏阴性细菌菌株，包括临床相关病原体，如甲氧西林耐金黄色葡萄球菌（MRSA）和S. ePidermidis 。肽肌瘤和扫描电子显微镜的肽瘤治疗MRSA确认膜活性作用模式。这些类似物在MIC水平下也显示出强烈的抗抗体活性，并在0.5-2％w / v水凝胶中证明了成熟MRSA的可存活率降低了> 50％的生物膜。此外，纳米纤维既不是细胞毒性，也不是溶血性。具有设计纳米结构与细菌的选择性的选择性模式，这些水凝胶可能对MRSA伤口感染和植入生物材料进行潜在的治疗方法。

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  • 来源
    《RSC Advances》 |2016年第113期|共11页
  • 作者

    Dewangan Rikeshwer Prasad; Jain Aditi; Tanwar Swati; Yar Mohammad Shahar; Pasha Santosh;

  • 作者单位

    CSIR Inst Genom &

    Integrat Biol Peptide Res Lab Mall Rd Delhi 110007 India;

    CSIR Inst Genom &

    Integrat Biol Peptide Res Lab Mall Rd Delhi 110007 India;

    CSIR Inst Genom &

    Integrat Biol Peptide Res Lab Mall Rd Delhi 110007 India;

    Jamia Hamdard Fac Pharm Dept Pharmaceut Chem New Delhi 110062 India;

    CSIR Inst Genom &

    Integrat Biol Peptide Res Lab Mall Rd Delhi 110007 India;

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  • 正文语种 eng
  • 中图分类 化学;
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