Photosensitizer-Polypeptide Conjugate with Synergistic Antibacterial Efficacy,Macromolecular Bioscience

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Photosensitizer-Polypeptide Conjugate with Synergistic Antibacterial Efficacy
Macromolecular Bioscience ( IF 4.4 ) Pub Date : 2022-05-08 , DOI: 10.1002/mabi.202200105
Pengqi Wan _{1,

2} , Wei Guo _{1,

2} , Yuxiu Duan _{1,

2} , Mingxiao Deng ₁ , Chunsheng Xiao _{2,

3}

Affiliation

Recently, continuous emergence of resistant bacteria has appeared as one of the most serious threats to human health. Therefore, systematic exploration of new antibacterial materials is of guiding significance. In this study, a series of photosensitizer-polypeptide conjugate (PPa-cP) is readily synthesized through simple ring-opening reactions to realize the synergistic antibacterial effects on Staphylococcus aureus (S. aureus) and methicillin-resistant S. aureus (MRSA) under light irradiation. Compared with free PPa, the cationic PPa-cP shows enhanced binding ability with the negative surface of S. aureus through electrostatic interaction, exhibiting effective antibacterial activity against both S. aureus and MRSA in vitro under light irradiation. Among the synthesized PPa-cP, PPa-cP5 with the degree of polymerization of 37 and modified with a 1-methylimidazole side group exhibits the best antibacterial activity with a minimum inhibitory concentration value of 2 µm without light irradiation and 0.25 µm with light irradiation. Moreover, PPa-cP5 shows good hemocompatibility. The above-mentioned results elucidate that the positively charged PPa-cP5 can significantly increase the efficiency of photodynamic therapy and effectively eradicate S. aureus biofilm due to its potent penetration ability into S. aureus biofilms. Overall, the present study establishes an efficient strategy for the treatment of S. aureus and S. aureus biofilm infections.

中文翻译：

具有协同抗菌功效的光敏剂-多肽缀合物

最近，耐药细菌的不断出现已成为对人类健康最严重的威胁之一。因此，系统探索新型抗菌材料具有指导意义。本研究通过简单的开环反应轻松合成了一系列光敏剂-多肽偶联物（PPa-cP），实现了对金黄色葡萄球菌（S. aureus）和耐甲氧西林金黄色葡萄球菌（MRSA）的协同抗菌作用。光照射。与游离PPa相比，阳离子PPa-cP通过静电作用增强了与金黄色葡萄球菌负表面的结合能力，对金黄色葡萄球菌均表现出有效的抗菌活性。和 MRSA 在体外光照射下。在合成的PPa-cP中，聚合度为37并经1-甲基咪唑侧基修饰的PPa-cP5表现出最好的抑菌活性，在光照条件下最低抑菌浓度值为2 µm，光照下最低抑菌浓度值为0.25 µm辐照。此外，PPa-cP5显示出良好的血液相容性。上述结果表明，带正电荷的PPa-cP5由于其对金黄色葡萄球菌生物膜的强大渗透能力，可以显着提高光动力治疗的效率并有效根除金黄色葡萄球菌生物膜。总体而言，本研究建立了治疗金黄色葡萄球菌的有效策略和金黄色葡萄球菌生物膜感染。

更新日期：2022-05-08

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