Pentacyclic triterpenoids from Freziera sp. that inhibit DNA polymerase β

Jing Zhen Deng, Shelley R. Starck, Sidney M. Hecht

Research output: Contribution to journalArticlepeer-review

31 Scopus citations

Abstract

In a survey of crude plant extracts for DNA polymerase β inhibitors, a methyl ethyl ketone extract prepared from Freziera sp. exhibited potent inhibition of DNA polymerase β. Bioassay-guided fractionation of the extract, guided by an assay to detect DNA polymerase β inhibition, resulted in the isolation of six active pentacyclic triterpenoids (1-6). These triterpenoids had IC50 values ranging from 7.5 to 16 μM in the presence of bovine serum albumin (BSA) and 2.6-5.8 μM in the absence of BSA, consistent with the possibility that these inhibitors may be of use in vivo. (C) 2000 Elsevier Science Ltd.

Original languageEnglish (US)
Pages (from-to)247-250
Number of pages4
JournalBioorganic and Medicinal Chemistry
Volume8
Issue number1
DOIs
StatePublished - Jan 1 2000
Externally publishedYes

Keywords

  • Chemotherapy
  • Enzyme inhibitors
  • Nucleic acids
  • Terpenes and terpenoids

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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