Influence of usnic acid and its derivatives on the activity of mammalian poly(ADP-ribose)polymerase 1 and DNA polymerase β

Med Chem. 2012 Sep;8(5):883-93. doi: 10.2174/157340612802084225.


The influence of a number of usnic acid derivatives on auto(polyADP-ribosyl)ation catalyzed by PARP1 and DNA synthesis catalyzed by DNA polymerase β was studied. The derivatives of usnic acid containing aromatic substituents were shown to be moderate inhibitors of PARP1. The presence of both usnic acid tricyclic structure and aromatic substituent at any position of the molecule is a key factor for the inhibitory action. In the case of DNA polymerase β, no relationship between the structure and inhibitory properties has been found with the only exception. Derivatives with modified ring A showed mild activation of DNA synthesis catalyzed by DNA polymerase β.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzofurans / chemical synthesis*
  • Benzofurans / pharmacology
  • Cell Line
  • Cell Survival / drug effects
  • DNA / antagonists & inhibitors*
  • DNA / biosynthesis
  • DNA Polymerase beta / antagonists & inhibitors*
  • DNA Polymerase beta / chemistry
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Kinetics
  • Mice
  • Molecular Structure
  • Poly (ADP-Ribose) Polymerase-1
  • Poly(ADP-ribose) Polymerase Inhibitors*
  • Poly(ADP-ribose) Polymerases / chemistry
  • Recombinant Proteins / antagonists & inhibitors
  • Recombinant Proteins / chemistry


  • Benzofurans
  • Enzyme Inhibitors
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Recombinant Proteins
  • usnic acid
  • DNA
  • PARP1 protein, human
  • Poly (ADP-Ribose) Polymerase-1
  • Poly(ADP-ribose) Polymerases
  • DNA Polymerase beta