Pentacyclic triterpenoids from Freziera sp. that inhibit DNA polymerase beta

Bioorg Med Chem. 2000 Jan;8(1):247-50. doi: 10.1016/s0968-0896(99)00276-x.

Abstract

In a survey of crude plant extracts for DNA polymerase 1 inhibitors, a methyl ethyl ketone extract prepared from Freziera sp. exhibited potent inhibition of DNA polymerase beta. Bioassay-guided fractionation of the extract, guided by an assay to detect DNA polymerase beta inhibition, resulted in the isolation of six active pentacyclic triterpenoids (1-6). These triterpenoids had IC50 values ranging from 7.5 to 16 microM in the presence of bovine serum albumin (BSA) and 2.6-5.8 microM in the absence of BSA, consistent with the possibility that these inhibitors may be of use in vivo.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Bleomycin / pharmacology
  • Cell Line
  • DNA Polymerase beta / antagonists & inhibitors*
  • Drug Synergism
  • Ericales / chemistry*
  • Molecular Structure
  • Triterpenes / chemistry
  • Triterpenes / isolation & purification
  • Triterpenes / pharmacology*

Substances

  • Triterpenes
  • Bleomycin
  • DNA Polymerase beta