Screening of Triterpenoids Isolated from Phyllanthus flexuosus for DNA Topoisomerase Inhibitory Activity
- 8 November 2001
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Natural Products
- Vol. 64 (12) , 1545-1547
- https://doi.org/10.1021/np010176u
Abstract
DNA topoisomerases (Topos) are enzymes that play a crucial role in DNA metabolism events such as replication, transcription, recombination, and chromosome segregation at mitosis. Thus, Topo inhibitors could be expected to have antitumor effects. Naturally occurring lupane- and oleanane-type triterpenoids isolated from the bark of Phyllanthus flexuosus were screened for human Topos I and II inhibitory activities. Olean-12-en-3β,15α-diol (1), olean-12-en-3β,15α,24-triol (3), lupeol (4), and betulin (6) were found to be selective catalytic inhibitors of human Topo II activity with IC50 values in the range of 10−39 μM.Keywords
This publication has 1 reference indexed in Scilit:
- Novel triterpenoids inhibit both DNA polymerase and DNA topoisomeraseBiochemical Journal, 2000