DNA polymerase β inhibitors from Baeckea gunniana

Jing Zhen Deng, Shelley R. Starck, Sidney Hecht

Research output: Contribution to journalArticle

43 Citations (Scopus)

Abstract

Crude plant extracts were surveyed for their ability to inhibit DNA polymerase β. A methyl ethyl ketone extract prepared from Baeckea gunniana was identified as a potent inhibitor of the enzyme. Bioassay-guided fractionation of the extract, using an assay to monitor the inhibitory potential of individual fractions toward DNA polymerase β, led to the isolation of four active ursane and oleanane triterpenoids (1-4). Inhibitory principle 1 is a new natural product, and 2 is a novel compound. Their structures were established as 3β-hydroxyurs-12,19(29)-dien-28- oic acid (1) and 3β-hydroxyurs-18,20(30)-dien-28-oic acid (2) by spectroscopic analysis and by comparison with the data for the structurally related compound ursolic acid (4). Also isolated as a DNA polymerase β inhibitor was oleanolic acid (3). Compounds 1-4 had IC50 values of 5.3-8.5 μM as inhibitors of polymerase β in the presence of bovine serum albumin (BSA) and 2.5-4.8 μM in the absence of BSA.

Original languageEnglish (US)
Pages (from-to)1624-1626
Number of pages3
JournalJournal of Natural Products
Volume62
Issue number12
DOIs
StatePublished - Dec 1999
Externally publishedYes

Fingerprint

Nucleic Acid Synthesis Inhibitors
DNA-directed DNA polymerase
DNA-Directed DNA Polymerase
Bovine Serum Albumin
bovine serum albumin
Oleanolic Acid
Acids
Spectroscopic analysis
Bioassay
Plant Extracts
Enzyme Inhibitors
Fractionation
Biological Products
Complex Mixtures
Biological Assay
Inhibitory Concentration 50
ursolic acid
Assays
oleanolic acid
enzyme inhibitors

ASJC Scopus subject areas

  • Plant Science
  • Chemistry (miscellaneous)
  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

Cite this

DNA polymerase β inhibitors from Baeckea gunniana. / Deng, Jing Zhen; Starck, Shelley R.; Hecht, Sidney.

In: Journal of Natural Products, Vol. 62, No. 12, 12.1999, p. 1624-1626.

Research output: Contribution to journalArticle

Deng, Jing Zhen ; Starck, Shelley R. ; Hecht, Sidney. / DNA polymerase β inhibitors from Baeckea gunniana. In: Journal of Natural Products. 1999 ; Vol. 62, No. 12. pp. 1624-1626.
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