期刊
MOLECULES
卷 24, 期 7, 页码 -出版社
MDPI
DOI: 10.3390/molecules24071319
关键词
phloretin; plant natural product; Propionibacterium acnes; inflammation; antimicrobial activity
资金
- National Research Foundation of Korea - Korean government [MSIP-2016R1A2B2008543]
- Technology Development Program - Ministry of SMEs and Startups (MSS, Korea) [s2609773]
- Korea Technology & Information Promotion Agency for SMEs (TIPA) [S2609773] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Phloretin is a natural chalcone with antibacterial and anti-inflammatory effects. This study investigated the anti-acne activity of phloretin against Propionibacterium acnes-induced skin infection and the potential target proteins of its anti-inflammatory and antibacterial effects. Phloretin potently inhibited the growth of P. acnes and P. acnes-induced Toll-like receptor (TLR) 2-mediated inflammatory signaling in human keratinocytes. Secreted embryonic alkaline phosphatase assay confirmed that the anti-inflammatory activity of phloretin is associated with the P. acnes-stimulated TLR2-mediated NF-kappa B signaling pathway. Phloretin significantly decreased the level of phosphorylated c-Jun N-terminal kinase (JNK), showing a binding affinity of 1.184 x 10(-5) M-1. We also found that phloretin binds with micromolar affinity to P. acnes beta-ketoacyl acyl carrier protein (ACP) synthase III (KAS III), an enzyme involved in fatty acid synthesis. Conformation-sensitive native polyacrylamide gel electrophoresis showed that phloretin reduced KAS III-mediated 3-ketoacyl ACP production by over 66%. A docking study revealed that phloretin interacts with the active sites of JNK1 and KAS III, suggesting their involvement in P. acnes-induced inflammation and their potential as targets for the antibacterial activity of phloretin. These results demonstrate that phloretin may be useful in the prevention or treatment of P. acnes infection.
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