Screening of triterpenoids isolated from Phyllanthus flexuosus for DNA topoisomerase inhibitory activity.

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Wada S, Iida A, Tanaka R

Screening of triterpenoids isolated from Phyllanthus flexuosus for DNA topoisomerase inhibitory activity.

J Nat Prod. 2001 Dec;64(12):1545-7.

PubMed ID
11754608 [ View in PubMed
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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-3 beta,15 alpha-diol (1), olean-12-en-3 beta,15 alpha,24-triol (3), lupeol (4), and betulin (6) were found to be selective catalytic inhibitors of human Topo II activity with IC(50) values in the range of 10-39 microM.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
EtoposideDNA topoisomerase 2-alphaIC 50 (nM)50000N/AN/ADetails