2. Academic Validation
  3. Topoisomerase II inhibitors from the roots of Stellera chamaejasme L

Topoisomerase II inhibitors from the roots of Stellera chamaejasme L

  • Bioorg Med Chem. 2014 Aug 1;22(15):4198-203. doi: 10.1016/j.bmc.2014.05.042.
Li-Ping Liu 1,  Kun Han 2,  Wei Chen 1,  Ying-Ying Zhang 1,  Lin-Jiang Tong 2,  Ting Peng 2,  Hua Xie 3,  Jian Ding 4,  Hong-Bing Wang 5
Affiliations

Affiliations

  • 1 School of Life Science & Technology, Tongji University, Shanghai 200092, PR China.
  • 2 Division of Anti-Tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, PR China.
  • 3 Division of Anti-Tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, PR China. Electronic address: hxie@simm.ac.cn.
  • 4 Division of Anti-Tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, PR China. Electronic address: suozhang@mail.shcnc.ac.cn.
  • 5 School of Life Science & Technology, Tongji University, Shanghai 200092, PR China. Electronic address: hbwang@tongji.edu.cn.
PMID: 24931277 DOI: 10.1016/j.bmc.2014.05.042
Abstract

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 μM. 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.

Keywords

Apoptosis; Cytotoxic activity; Stellera chamaejasme L.; Topoisomerase II.

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