Chemical Biology and Drug Design
Chemical Biology and Drug Design
5 years ago

Preliminary investigations into developing all-D Omiganan for treating Mupirocin-resistant MRSA skin infections

Preliminary investigations into developing all-D Omiganan for treating Mupirocin-resistant MRSA skin infections
Qiu Ying Lau, Roland Jureen, Fui Mee Ng, Siew Mei Samantha Ng, C. S. Brian Chia, Jeffrey Hill, Shu Wei Teo, Yaqing Elena Yong
Staphylococcus aureus is the primary pathogen responsible for the majority of human skin infections, and meticillin-resistant S. aureus (MRSA) currently presents a major clinical concern. The overuse of Mupirocin, the first-line topical antibacterial drug over 30 years, has led to the emergence of Mupirocin-resistant MRSA, creating a clinical concern. The antimicrobial peptide Omiganan was touted to be a promising antibacterial drug candidate due to its rapid membrane-disrupting bactericidal mode of action, entering clinical trials in 2005 as a topical gel to prevent catheter site infections. However, drug development ceased in 2009 due to a lack of efficacy. We postulate this to be due to proteolytic degradation caused by endogenous human skin proteases. Herein, we tested our hypothesis using Omiganan and its all-D enantiomer in a human skin protease stability assay, followed by anti-MRSA activity assay against of a panel of clinical MRSA isolates, a bactericidal/static determination and a time-kill assay to gauge all-D Omiganan's potential for further topical antibacterial drug development. Herein, we compared the skin protease stability and antibacterial activity of Omiganan, an antimicrobial peptide, to its all-D enantiomer. Results revealed that the latter was proteolytically more stable while possessing the same antibacterial potency, suggesting that the all-D peptide may be better suited as a topical drug development candidate.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1111/cbdd.13035

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