Pterostilbene, a methoxylated resveratrol derivative, efficiently eradicates planktonic, biofilm, and intracellular MRSA by topical application

Shih Chun Yang, Chih Hua Tseng, Pei Wen Wang, Po Liang Lu, Yi Han Weng, Feng Lin Yen*, Jia You Fang

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

60 Scopus citations

Abstract

Pterostilbene is a methoxylated derivative of resveratrol originated from natural sources. We investigated the antibacterial activity of pterostilbene against drug-resistant Staphylococcus aureus and the feasibility of using it to treat cutaneous bacteria. The antimicrobial effect was evaluated using an in vitro culture model and an in vivo mouse model of cutaneous infection. The minimum inhibitory concentration (MIC) assay demonstrated a superior biocidal activity of pterostilbene compared to resveratrol (8~16-fold) against methicillin-resistant S. aureus (MRSA) and clinically isolated vancomycin-intermediate S. aureus (VISA). Pterostilbene was found to reduce MRSA biofilm thickness from 18 to 10 μm as detected by confocal microscopy. Pterostilbene showed minimal toxicity to THP-1 cells and was readily engulfed by the macrophages, facilitating the eradication of intracellular MRSA. Pterostilbene exhibited increased skin absorption over resveratrol by 6-fold. Topical pterostilbene application improved the abscess formation produced by MRSA by reducing the bacterial burden and ameliorating the skin architecture. The potent anti-MRSA capability of pterostilbene was related to bacterial membrane leakage, chaperone protein downregulation, and ribosomal protein upregulation. This mechanism of action was different from that of resveratrol according to proteomic analysis and molecular docking. Pterostilbene has the potential to serve as a novel class of topically applied agents for treating MRSA infection in the skin while demonstrating less toxicity to mammalian cells.

Original languageEnglish
Article number1103
JournalFrontiers in Microbiology
Volume8
Issue numberJUN
DOIs
StatePublished - 13 06 2017

Bibliographical note

Publisher Copyright:
© 2017 Yang, Tseng, Wang, Lu, Weng, Yen and Fang.

Keywords

  • Biofilm
  • MRSA
  • Proteomics
  • Pterostilbene
  • Resveratrol
  • Skin infection

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