Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 22, Issue 15, Pages 4198-4203Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.05.042
Keywords
Stellera chamaejasme L.; Cytotoxic activity; Topoisomerase II; Apoptosis
Funding
- National Natural Science Foundation [81001369, 31170327, 81173080, 81321092]
- Fundamental Research Funds for the Central Universities of the People's Republic of China
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Three new compounds, including one daphnane diterpene (1), one sesquiterpene (6), and one lignan (7) have been isolated from the Stellera chamaejasme L., together with five other known compounds, including four daphnane diterpenenoids (2-5) and one lignan (8). The structures of the new compounds were elucidated by spectroscopic analysis. The cytotoxicities of compounds 1-8 towards human lung adenocarcinoma cells (A549 cells) were evaluated using a sulforhodamine B assay. All of the compounds displayed significant cytotoxicity, with IC50 values in the ranging of 0.2 nM to 2.0 mu M. Mechanistic studies revealed that the antitumor activities of compounds 1-3 and 7 were derived from their inhibition of topoisomerase II (Topo II). Furthermore, as a Topo II inhibitor, compound 1 was found to effectively induced G2-M phase cell cycle arrest and apoptosis in cancer cells. (C) 2014 Elsevier Ltd. All rights reserved.
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