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<p>The development of advanced antibacterial materials to combat multidrug-resistant pathogens remains a significant challenge in the healthcare sector. Herein, we report the design and synthesis of a novel pillar[5]arene-based platinum metallacycle (<b>P5Pt</b>) specifically engineered to combat multidrug-resistant pathogens such as methicillin-resistant <i>Staphylococcus aureus</i> (MRSA). The obtained metallacycle serves as a host molecule that can bind with an ethylene glycol-linked bis-biotin diester linker, resulting in a water-soluble supramolecular nanosystem (<b>P5Pt-Bio</b>). Both <b>P5Pt</b> and <b>P5Pt-Bio</b> demonstrate remarkable efficacy against drug-resistant bacteria, particularly MRSA, with minimum inhibitory concentrations of 3.1 µM for <b>P5Pt-Bio</b>. Mechanistic investigations, including scanning electron microscopy and protein leakage assays, reveal significant disruption of bacterial membranes, ultimately leading to bacterial cell death. Notably, <b>P5Pt-Bio</b> displays excellent biocompatibility with human keratinocyte cells. These findings underscore the potential of pillar[5]arene-based supramolecular nanosystems as versatile platforms for antibacterial applications.</p>

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Pillararene-based AIE-active metallacycle for efficient eradication of antibiotic-resistant bacteria

  • 期刊论文

  • 发表日期：

    2025年9月17日

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  • Ponmani Jeyakkumar,
  • Kehan Du,
  • Rongbo Zhang,
  • Xueqi Tian,
  • Qian Liu,
  • Jianmin Jiao,
  • Hao Jiang,
  • Xiujun Yu,
  • Xiao-Yu Hu

摘要

The development of advanced antibacterial materials to combat multidrug-resistant pathogens remains a significant challenge in the healthcare sector. Herein, we report the design and synthesis of a novel pillar[5]arene-based platinum metallacycle (P5Pt) specifically engineered to combat multidrug-resistant pathogens such as methicillin-resistant Staphylococcus aureus (MRSA). The obtained metallacycle serves as a host molecule that can bind with an ethylene glycol-linked bis-biotin diester linker, resulting in a water-soluble supramolecular nanosystem (P5Pt-Bio). Both P5Pt and P5Pt-Bio demonstrate remarkable efficacy against drug-resistant bacteria, particularly MRSA, with minimum inhibitory concentrations of 3.1 µM for P5Pt-Bio. Mechanistic investigations, including scanning electron microscopy and protein leakage assays, reveal significant disruption of bacterial membranes, ultimately leading to bacterial cell death. Notably, P5Pt-Bio displays excellent biocompatibility with human keratinocyte cells. These findings underscore the potential of pillar[5]arene-based supramolecular nanosystems as versatile platforms for antibacterial applications.