Unbiased screening of marine sponge extracts for anti-inflammatory agents combined with chemical genomics identifies girolline as an inhibitor of protein synthesis

ACS Chem Biol. 2014 Jan 17;9(1):247-57. doi: 10.1021/cb400740c. Epub 2013 Oct 29.

Abstract

Toll-like receptors (TLRs) play a critical role in innate immunity, but activation of TLR signaling pathways is also associated with many harmful inflammatory diseases. Identification of novel anti-inflammatory molecules targeting TLR signaling pathways is central to the development of new treatment approaches for acute and chronic inflammation. We performed high-throughput screening from crude marine sponge extracts on TLR5 signaling and identified girolline. We demonstrated that girolline inhibits signaling through both MyD88-dependent and -independent TLRs (i.e., TLR2, 3, 4, 5, and 7) and reduces cytokine (IL-6 and IL-8) production in human peripheral blood mononuclear cells and macrophages. Using a chemical genomics approach, we identified Elongation Factor 2 as the molecular target of girolline, which inhibits protein synthesis at the elongation step. Together these data identify the sponge natural product girolline as a potential anti-inflammatory agent acting through inhibition of protein synthesis.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / isolation & purification*
  • Anti-Inflammatory Agents / pharmacology*
  • CHO Cells
  • Cells, Cultured
  • Cricetulus
  • Drug Evaluation, Preclinical
  • Humans
  • Imidazoles / isolation & purification*
  • Imidazoles / pharmacology*
  • Interleukin-6 / immunology
  • Interleukin-8 / immunology
  • Leukocytes, Mononuclear / drug effects
  • Leukocytes, Mononuclear / immunology
  • Macrophages / drug effects
  • Macrophages / immunology
  • Myeloid Differentiation Factor 88 / immunology
  • Porifera / chemistry*
  • Protein Biosynthesis / drug effects*
  • Toll-Like Receptors / immunology

Substances

  • Anti-Inflammatory Agents
  • Imidazoles
  • Interleukin-6
  • Interleukin-8
  • Myeloid Differentiation Factor 88
  • Toll-Like Receptors
  • girolline