The resveratrol tetramer (-)-hopeaphenol inhibits type III secretion in the gram-negative pathogens Yersinia pseudotuberculosis and Pseudomonas aeruginosa

PLoS One. 2013 Dec 4;8(12):e81969. doi: 10.1371/journal.pone.0081969. eCollection 2013.

Abstract

Society faces huge challenges, as a large number of bacteria have developed resistance towards many or all of the antibiotics currently available. Novel strategies that can help solve this problem are urgently needed. One such strategy is to target bacterial virulence, the ability to cause disease e.g., by inhibition of type III secretion systems (T3SSs) utilized by many clinically relevant gram-negative pathogens. Many of the antibiotics used today originate from natural sources. In contrast, most virulence-blocking compounds towards the T3SS identified so far are small organic molecules. A recent high-throughput screening of a prefractionated natural product library identified the resveratrol tetramer (-)-hopeaphenol as an inhibitor of the T3SS in Yersinia pseudotuberculosis. In this study we have investigated the virulence blocking properties of (-)-hopeaphenol in three different gram-negative bacteria. (-)-Hopeaphenol was found to have micromolar activity towards the T3SSs in Yersinia pseudotuberculosis and Pseudomonas aeruginosa in cell-based infection models. In addition (-)-hopeaphenol reduced cell entry and subsequent intracellular growth of Chlamydia trachomatis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bacterial Proteins / metabolism*
  • Bacterial Secretion Systems / drug effects*
  • Blotting, Western
  • Chlamydia trachomatis / drug effects
  • Chlamydia trachomatis / growth & development
  • HeLa Cells
  • Humans
  • Phenols
  • Protein Transport / drug effects
  • Pseudomonas aeruginosa / drug effects*
  • Pseudomonas aeruginosa / growth & development
  • Pseudomonas aeruginosa / metabolism
  • Pseudomonas aeruginosa / pathogenicity
  • Resveratrol
  • Stilbenes / chemistry
  • Stilbenes / pharmacology*
  • Virulence / drug effects
  • Yersinia pseudotuberculosis / drug effects*
  • Yersinia pseudotuberculosis / growth & development
  • Yersinia pseudotuberculosis / metabolism

Substances

  • Bacterial Proteins
  • Bacterial Secretion Systems
  • Phenols
  • Stilbenes
  • hopeaphenol
  • Resveratrol

Grants and funding

Funding provided by the Swedish Research Council, www.vr.se, The Kempe Foundations, www.kempe.com, The Australian Research Council (linkage grant # LP120200339, ARC Grant LE0668477 and LE0237908). The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.