Retracted: Short lipopeptides specifically inhibit the growth of Propionibacterium acnes with dual antibacterial and anti‐inflammatory action

Abstract

Background and Purpose: Propionibacterium acnes (P. acnes) is a Gram-positive bacterium associated with the skin disorder acne. In this study, we determined the importance of fatty acids 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: Antimicrobial activity was determined by the minimal inhibitory concentration (MIC). Lipids from P. acnes were used to explore the mode of action. RAW264.7 cells respectively stimulated with LPS and P. acnes were used to measure the 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, with an MIC of 2 μg•ml −1 , 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 bacterial membrane, thereby impairing membrane permeability and causing leakage of the inner contents of bacterial cells. In addition, 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 assessed in animal studies in vivo. Conclusions and Implications: C16-KWKW is a lipopeptide displaying both anti-P. acnes and anti-inflammatory effects in vitro and in vivo, and exhibits potential as a treatment for acne vulgaris induced by P. acnes. 1 | INTRODUCTION Acne vulgaris is a chronic skin disorder that often develops on the face and upper trunk and is characterized by the formation of comedones, papules, nodules, pustules, and cysts (Aslam, Fleischer, & Feldman, 2015). In addition, the disease is always associated with an emotional and psychological impact, which can result in anxiety, reduced selfesteem, and depression or even thoughts of suicide (Tasoula et al., 2012). It affected more than 630 million people globally in 2015, thus being ranked as the eighth most common disease in the world (Disease, Injury, & Prevalence, 2016). Current research shows that several factors are involved in the development of this condition including an overgrowth of the skin commensal bacteria, obstruction of the follicle, excess production of sebum, and inflammation of the

Suppression of Cutibacterium acnes-Mediated Inflammatory Reactions by Fibroblast Growth Factor 21 in Skin

“…Acne may be relieved by the administration of several exogenous drugs. Some small peptides, such as melittin and short lipopeptides, can protect cells from inflammatory responses induced by C. acnes and may even have direct antibacterial effects [ 48 ]. Several biologically active compounds extracted from plants have been found to inhibit the occurrence of acne to varying degrees [ 49 , 50 , 51 , 52 ].…”

Anti-Toxoplasma gondii Effects of Lipopeptide Derivatives of Lycosin-I

“…To improve the structural stability and activity of the peptide, its structure is modified via various methods including acetylation, amidation, amino acid replacement, D-amino acid substitution, the deletion of inactive amino acids, cyclization into a cyclic peptide, and fatty acid modification into a lipopeptide. Recent studies have shown that cyclic peptides and lipopeptides can enhance the biological activity and stability of peptides [ 32 , 33 , 34 , 35 ]. Fatty acids, a class of essential nutrients, regulate a wide range of vital processes and disorders including diabetes, cancer, and cardiovascular disease [ 36 , 37 ].…”