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<p>Despite decades of investigation, multidrug-resistant bacterial resistance has become the leading health concern globally related to MRSA infections, where conventional antibiotics have failed in this race. However, the development of short cationic antimicrobial peptides with higher efficacy and low cytotoxicity has encouraged our recent exploration. Herein, we describe the synthesis, characterization, and antibacterial evaluation of tetrahydropiperic acid (THPA) conjugate αβ-hybrid peptides, THPA-Lys-<i>tBu</i>-β<sup>3,3</sup>Ac<sub>6</sub>c-PEA, <b>P1</b>; THPA-Orn-<i>tBu</i>-β<sup>3,3</sup>Ac<sub>6</sub>c-PEA, <b>P2</b>, and THPA-Arg-<i>tBu</i>-β<sup>3,3</sup>Ac<sub>6</sub>c-PEA, <b>P3</b>. Our investigation revealed peptide <b>P3</b> exhibited low hemolytic and best safety index along with higher bactericidal potency against MRSA. Combinatorial study with vancomycin suggested synergistic effect. Mechanistic investigations revealed membrane disruption of MRSA by the peptide. This study suggested that peptide <b>P3</b> could be an effective therapeutic option to resist the emergence of MRSA-related infections.</p>

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Antibacterial activity and mechanism of optimized THPA conjugated dipeptides against methicillin-resistant Staphylococcus aureus

  • 期刊论文

  • 发表日期：

    2025年11月10日

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  • Arti Rathore,
  • Beenish Rashid,
  • Aminur Rahman Sarkar,
  • Shifa Firdous,
  • Rubina Chowdhary,
  • Rakshit Manhas,
  • Faizan Ahmad Magray,
  • Biplab Sarkar,
  • Jyoti Kumari,
  • Rajkishor Rai,
  • Avisek Mahapa

摘要

Despite decades of investigation, multidrug-resistant bacterial resistance has become the leading health concern globally related to MRSA infections, where conventional antibiotics have failed in this race. However, the development of short cationic antimicrobial peptides with higher efficacy and low cytotoxicity has encouraged our recent exploration. Herein, we describe the synthesis, characterization, and antibacterial evaluation of tetrahydropiperic acid (THPA) conjugate αβ-hybrid peptides, THPA-Lys-tBu-β3,3Ac6c-PEA, P1; THPA-Orn-tBu-β3,3Ac6c-PEA, P2, and THPA-Arg-tBu-β3,3Ac6c-PEA, P3. Our investigation revealed peptide P3 exhibited low hemolytic and best safety index along with higher bactericidal potency against MRSA. Combinatorial study with vancomycin suggested synergistic effect. Mechanistic investigations revealed membrane disruption of MRSA by the peptide. This study suggested that peptide P3 could be an effective therapeutic option to resist the emergence of MRSA-related infections.