Activity-guided screening of bioactive natural compounds implementing a new glucocorticoid-receptor-translocation assay and detection of new anti-inflammatory steroids from bacteria

Biotechnol Lett. 2013 Jan;35(1):11-20. doi: 10.1007/s10529-012-1042-0. Epub 2012 Sep 15.

Abstract

Using an in vitro cell-based assay in a flow-design, we have applied activity-guided screening to search for new bioactive compounds isolated from microorganisms. A first assay employs the stable expression of nuclear factor kappa B (NF-κB) while a second assay utilizes the glucocorticoid receptor (GR) coupled to green fluorescent protein. A specialized assay was implemented for both the translocation of NF-κB and to inhibit the translocation of cytokine-mediated NF-κB. In addition, we developed in a wide palette of cell lines used for a highly specialized GR-translocation assay to detect anti-inflammatory effects. This approach demonstrates the straight-forward combination of cell-based assays arranged with an automated fluorescence microscope. This allows for the direct sorting of extracts which are acting in a pharmaceutically interesting way. Initial results using this technique have led to the detection of new anti-inflammatory steroids from bacterial crude extracts.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / metabolism
  • Anti-Inflammatory Agents / pharmacology*
  • Biological Assay / methods*
  • Biological Products / metabolism
  • Biological Products / pharmacology*
  • CHO Cells
  • Cell Line
  • Cricetinae
  • Cricetulus
  • Drug Evaluation, Preclinical / methods*
  • Green Fluorescent Proteins / genetics
  • Green Fluorescent Proteins / metabolism
  • Hydroxysteroids / metabolism
  • Hydroxysteroids / pharmacology*
  • Mice
  • NF-kappa B / genetics
  • NF-kappa B / metabolism
  • Reactive Oxygen Species / metabolism
  • Receptors, Glucocorticoid / genetics
  • Receptors, Glucocorticoid / metabolism*
  • Transfection

Substances

  • Anti-Inflammatory Agents
  • Biological Products
  • Hydroxysteroids
  • NF-kappa B
  • Reactive Oxygen Species
  • Receptors, Glucocorticoid
  • Green Fluorescent Proteins