Identification of a naturally occurring quinazolin-4(3H)-one firefly luciferase inhibitor

J Nat Prod. 2011 Jun 24;74(6):1500-2. doi: 10.1021/np1006179. Epub 2011 Jun 3.

Abstract

A prefractionated Streptomyces-derived extract was initially identified as being active using a luciferase-based AMP-activated protein kinase (AMPK) assay. Bioassay-guided fractionation led to the isolation of the new compound quinazolin-4(3H)-one (1) as the active component. However, 1 was shown to have potent firefly luciferase inhibitory activity with no effect on AMPK. This is the first report of a natural luciferase inhibitor.

MeSH terms

  • AMP-Activated Protein Kinases / metabolism*
  • Animals
  • Biological Products / chemistry
  • Biological Products / isolation & purification*
  • Biological Products / pharmacology*
  • Luciferases, Firefly / antagonists & inhibitors*
  • Luciferases, Firefly / metabolism
  • Molecular Structure
  • Quinazolinones / chemistry
  • Quinazolinones / isolation & purification*
  • Quinazolinones / pharmacology*
  • Streptomyces / chemistry*

Substances

  • 2-(4'-(methylamino)phenyl)quinazolin-4(3H)-one
  • Biological Products
  • Quinazolinones
  • Luciferases, Firefly
  • AMP-Activated Protein Kinases