2. Academic Validation
  3. Lipidated α/Sulfono-α-AA heterogeneous peptides as antimicrobial agents for MRSA

Lipidated α/Sulfono-α-AA heterogeneous peptides as antimicrobial agents for MRSA

  • Bioorg Med Chem. 2020 Jan 1;28(1):115241. doi: 10.1016/j.bmc.2019.115241.
Sylvia Singh 1,  Minghui Wang 1,  Ruixuan Gao 1,  Peng Teng 1,  Timothy Odom 1,  En Zhang 2,  Hai Xu 3,  Jianfeng Cai 4
Affiliations

Affiliations

  • 1 Department of Chemistry, University of South Florida, 4202 East Fowler Avenue, Tampa, FL 33620, United States.
  • 2 Department of Chemistry, University of South Florida, 4202 East Fowler Avenue, Tampa, FL 33620, United States; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China.
  • 3 College of Chemistry and Chemical Engineering, Central South University, Changsha 410083, PR China.
  • 4 Department of Chemistry, University of South Florida, 4202 East Fowler Avenue, Tampa, FL 33620, United States. Electronic address: hshim@emory.edu.
PMID: 31812324 DOI: 10.1016/j.bmc.2019.115241
Abstract

Though Antibiotics have been used for decades to treat Bacterial infections, there is a great need for new treatment methods. Bacteria are becoming resistant to conventional Antibiotics, as is the case with Methicillin resistant Staphylococcus aureus (MRSA). Herein we report the design of a series of lipidated α/Sulfono-α-AA heterogeneous Peptides as mimics for Host Defense Peptides (HDPs). Utilizing fluorescence microscopy and depolarization techniques, our compounds demonstrate the ability to kill Gram-positive bacteria through cell membrane disruption. This mechanism of action makes it difficult for bacteria to develop resistance. Further time kill studies and hemolytic assays have also proven these compounds to be efficient in their ability to eradicate bacteria cells while remaining non-toxic to human red blood cells. This new class of peptidomimetics shows promise for the future Antibiotic treatment of MRSA.

Keywords

Antimicrobial; Bacterial resistance; Host Defense Peptides; Lipidation; Peptidomimetics.

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