Herein, we make an effort to enhance the antimicrobial activity of levofloxacin (LVX) antibiotic via conjugation to a cell‐penetrating peptide (CPP) including Cys‐Gly‐Ala‐Phe‐Pro‐His‐Arg. For this purpose, cysteine is used as a linker between the LVX and CPP chain, and two heterogeneous nanoscale catalytic systems are employed as the substantial alternatives for traditional peptide coupling reagents like N,N,N′,N′‐tetramethyl‐O‐(benzotriazol‐1‐yl)uronium tetrafluoroborate (TBTU). Briefly, it has been found out that the antimicrobial potency of the synthesized CPP‐LVX conjugate (on the gram‐positive and gram‐negative bacteria) is noticeably enhanced (~20% more). It has been revealed via zone of inhibition (ZOI) and optical density (OD) evaluations. As a convenient method for making this type of the effective conjugations, ultrasound waves (with a specific frequency and power density) activate the catalytic sites of the heterogeneous nanoparticles. Through this synergistic effect, peptide/amide bond is formed during a short time (10 min), and high reaction yield (>90%) is obtained under mild conditions. Moreover, as a simple purification process, the catalyst nanoparticles are collected and separated through their high magnetic property.

中文翻译：

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左氧氟沙星通过与细胞穿透肽结合的抗微生物治疗增强作用：一种有效的声化学催化过程。

在此，我们努力通过与包括Cys-Gly-Ala-Phe-Pro-His-Arg在内的细胞穿透肽（CPP）结合来增强左氧氟沙星（LVX）抗生素的抗菌活性。为此，将半胱氨酸用作LVX和CPP链之间的连接基，并且使用两种异质纳米级催化系统作为传统肽偶联剂（如N，N，N '，N）的基本替代品'-四甲基-O-（苯并三唑-1-基）四氟硼酸铀（TBTU）。简而言之，已发现合成的CPP-LVX共轭物（对革兰氏阳性和革兰氏阴性细菌）的抗菌效力显着提高（提高了约20％）。通过抑制区（ZOI）和光密度（OD）评估可以发现这一点。作为进行这种有效缀合的一种便捷方法，超声波（具有特定的频率和功率密度）可以激活异质纳米颗粒的催化位点。通过这种协同作用，在短时间内（10分钟）形成了肽/酰胺键，在温和条件下获得了很高的反应产率（> 90％）。此外，作为简单的纯化方法，催化剂纳米颗粒通过其高磁性而被收集和分离。