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 language | English (US) |
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Pages (from-to) | 247-250 |
Number of pages | 4 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 8 |
Issue number | 1 |
DOIs | |
State | Published - Jan 1 2000 |
Externally published | Yes |
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