Article date: July 2019
By: Guang Yang, Jingyu Wang, Shengsheng Lu, Zhao Chen, Sheng Fan, Daiwei Chen, Huanxin Xue, Wenyuan Shi, Jian He in Volume 176, Issue 13, pages 2321-2335
Background and Purpose
Propionibacterium acnes is a Gram‐positive bacterium associated with the skin disorder acne. In this study, as fatty acids are considered to be important in the life habitat of P. acnes, we tested our lipopeptide library in an attempt to create potent P. acnes‐specific antimicrobial agents.
Experimental Approach
The antimicrobial activity of various lipopeptides was determined by measuring their minimal inhibitory concentration (MIC). Lipids from P. acnes were used to explore their mode of action. RAW264.7 cells stimulated with LPS and P. acnes respectively were used to measure their anti‐inflammatory activity. Mice ears injected with P. acnes were used to assess the antimicrobial and anti‐inflammatory effects of the peptides tested in vivo.
Key Results
The most potent candidate, C16‐KWKW, was observed to be more active against P. acnes than against other non‐targeted bacterial strains, such as Streptococcus mutans, Staphylococcus aureus, and Escherichia coli. The mode of action of C16‐KWKW was observed to be through interference with the integrity of the bacterial membrane, thereby impairing membrane permeability and causing leakage of inner contents of bacterial cells. Furthermore, C16‐KWKW inhibited the expression of pro‐inflammatory cytokines, such as IL‐1β, TNF‐α, and inducible NOS stimulated by both LPS and P. acnes, thus showing potential anti‐inflammatory activity, which was further verified in the in vivo animal studies.
Conclusions and Implications
C16‐KWKW is a lipopeptide displaying both anti‐P. acnes and anti‐inflammatory effects in vitro and in vivo and shows potential as a treatment for acne vulgaris induced by P. acnes.
DOI: 10.1111/bph.14680
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