Therapeutic potential, antimicrobial activity against acne-causing bacteria, and modes of action of WKK10 and WRR10, novel cationic antimicrobial peptides
2
Issued Date
2025-10-01
Resource Type
ISSN
00452068
eISSN
10902120
Scopus ID
2-s2.0-105015108927
Journal Title
Bioorganic Chemistry
Volume
165
Rights Holder(s)
SCOPUS
Bibliographic Citation
Bioorganic Chemistry Vol.165 (2025)
Suggested Citation
Phosri S., Tastub S., Intharuksa A., Techarang T., Srisucharitpanit K., Hooper S.E., Theansungnoen T. Therapeutic potential, antimicrobial activity against acne-causing bacteria, and modes of action of WKK10 and WRR10, novel cationic antimicrobial peptides. Bioorganic Chemistry Vol.165 (2025). doi:10.1016/j.bioorg.2025.108965 Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/112041
Title
Therapeutic potential, antimicrobial activity against acne-causing bacteria, and modes of action of WKK10 and WRR10, novel cationic antimicrobial peptides
Corresponding Author(s)
Other Contributor(s)
Abstract
Although antimicrobial peptides possess potent antimicrobial activities, the high cost of production, based on amino acid length, has limited their therapeutic and cosmeceutical applications. This study aimed to produce and characterize de novo designed antimicrobial peptides derived from WSKK11 and WSRR11 for efficacy against acne-causing bacteria. Ten designed peptides were evaluated for antimicrobial, hemolytic, and cytotoxic activities, as well as, secondary structures by FTIR and modes of action. Of the ten peptides, WKK10, WWKK11, WRR10, and WRRR11 had antimicrobial activity against Cutibacterium acnes DMST 14916 at the minimum inhibitory concentrations (MICs) of 64, 16, 32, and 32 μg/mL, respectively. The MICs of WKK10, WWKK11, WSRR10, and WRRR11 against Staphylococcus aureus TISTR 746 were 8, 4, 16, and 16 μg/mL, while those against Staphylococcus epidermidis TISTR 518 were 8, 4, 32, and 16 μg/mL, respectively. These peptides were less toxic to human erythrocytes, and WWKK11 and WRRR11 had no toxicity for MRC-5 fibroblasts, with toxicity to RAW 264.7 macrophage (≥50 μg/mL) and HaCaT keratinocyte (≥100 μg/mL). WKK10 and WRR10 were not toxic to RAW 264.7, HaCaT, and MRC-5 cells up to 100 μg/mL. Beta-sheet and alpha-helix structures of the peptides were adopted predominantly in 20 mM Tris-HCl, pH 7.4 and 50% TFE, respectively. The peptides revealed direct activity and perturbation of the cell envelope, observed by scanning electron microscopy. The results indicate that the four novel peptides, particularly WKK10 and WRR10, are promising topical antimicrobial agents for acne treatment.