The Journal of antibiotics · 2025
Antibacterial activity and mechanism of optimized THPA conjugated dipeptides against methicillin-resistant Staphylococcus aureus.
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Rathore Arti, Rashid Beenish, Sarkar Aminur Rahman, Firdous Shifa, Chowdhary Rubina, Manhas Rakshit, Magray Faizan Ahmad, Sarkar Biplab, Kumari Jyoti, Rai Rajkishor, Mahapa Avisek
Аннотация
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.