Cytotoxic Pentacyclic Triterpenoids from Combretum sundaicum and Lantana camara as Inhibitors of Bcl-xL/BakBH3 Domain Peptide Interaction
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- 作者：Marc Litaudon ; Claire Jolly ; Catherine Le Callonec ; Dao Din Cuong ; Pascal Retailleau ; Olivier Nosjean ; Van Hung Nguyen ; Bruno Pfeiffer ; Jean A. Boutin ; Franoise Guritte
- 刊名：Journal of Natural Products
- 出版年：2009
- 出版时间：July 24, 2009
- 年：2009
- 卷：72
- 期：7
- 页码：1314-1320
- 全文大小：170K
- 年卷期：v.72,no.7(July 24, 2009)
- ISSN：1520-6025
文摘
In an effort to discover potent inhibitors of the antiapoptotic protein Bcl-xL, a systematic in vitro evaluation was undertaken on extracts prepared from various parts of Vietnamese plants. The ethyl acetate extracts obtained from the leaves and flowers of Combretum sundaicum and the leaves of Lantana camara were selected for their interaction with the Bcl-xL/Bak association. Bioassay-guided purification of these species led to the isolation of 15 pentacyclic triterpenoids (1−15) possessing olean-12-en-28-oic acid and olean-12-en-29-oic acid aglycons, of which compounds 1−6 and 8−10 are new. Five compounds exhibited binding activity with Ki values between 5.3 and 17.8 μM. The cytotoxic activity of 1−15 was also evaluated on various cancer cell lines.