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Open AccessArticle

Target Proteins of Phloretin for Its Anti-Inflammatory and Antibacterial Activities Against Propionibacterium acnes-Induced Skin Infection

1
Department of Bioscience and Biotechnology, Konkuk University, Seoul 05029, Korea
2
School of Systems Biomedical Science, Soongsil University, Seoul 06978, Korea
*
Author to whom correspondence should be addressed.
Academic Editor: Maria G. Miguel
Molecules 2019, 24(7), 1319; https://doi.org/10.3390/molecules24071319
Received: 27 February 2019 / Revised: 25 March 2019 / Accepted: 2 April 2019 / Published: 3 April 2019
(This article belongs to the Special Issue Anti-Inflammatory Activity of Natural Products)
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-κB signaling pathway. Phloretin significantly decreased the level of phosphorylated c-Jun N-terminal kinase (JNK), showing a binding affinity of 1.184 × 10−5 M−1. We also found that phloretin binds with micromolar affinity to P. acnes β-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. View Full-Text
Keywords: phloretin; plant natural product; Propionibacterium acnes; inflammation; antimicrobial activity phloretin; plant natural product; Propionibacterium acnes; inflammation; antimicrobial activity
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MDPI and ACS Style

Cheon, D.; Kim, J.; Jeon, D.; Shin, H.-C.; Kim, Y. Target Proteins of Phloretin for Its Anti-Inflammatory and Antibacterial Activities Against Propionibacterium acnes-Induced Skin Infection. Molecules 2019, 24, 1319. https://doi.org/10.3390/molecules24071319

AMA Style

Cheon D, Kim J, Jeon D, Shin H-C, Kim Y. Target Proteins of Phloretin for Its Anti-Inflammatory and Antibacterial Activities Against Propionibacterium acnes-Induced Skin Infection. Molecules. 2019; 24(7):1319. https://doi.org/10.3390/molecules24071319

Chicago/Turabian Style

Cheon, Dasom; Kim, Jieun; Jeon, Dasom; Shin, Hang-Cheol; Kim, Yangmee. 2019. "Target Proteins of Phloretin for Its Anti-Inflammatory and Antibacterial Activities Against Propionibacterium acnes-Induced Skin Infection" Molecules 24, no. 7: 1319. https://doi.org/10.3390/molecules24071319

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