Topoisomerase II inhibitors from the roots of Stellera chamaejasme L.
Liu, Li-Ping1; Han, Kun2; Chen, Wei1; Zhang, Ying-Ying1; Tong, Lin-Jiang2; Peng, Ting2; Xie, Hua2; Ding, Jian2; Wang, Hong-Bing1
刊名BIOORGANIC & MEDICINAL CHEMISTRY
2014-08-01
卷号22期号:15页码:4198-4203
关键词Stellera chamaejasme L. Cytotoxic activity Topoisomerase II Apoptosis
ISSN号0968-0896
DOI10.1016/j.bmc.2014.05.042
文献子类Article
英文摘要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.
资助项目National Natural Science Foundation[81001369] ; National Natural Science Foundation[31170327] ; National Natural Science Foundation[81173080] ; National Natural Science Foundation[81321092] ; Fundamental Research Funds for the Central Universities of the People's Republic of China[00000000]
WOS关键词POTENT ANTITUMOR ACTIVITIES ; PISCICIDAL CONSTITUENTS ; DAPHNANE DITERPENES ; APOPTOSIS ; DERIVATIVES ; COUMARINS ; AGENTS ; ARREST
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种英语
出版者PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号WOS:000339859700043
内容类型期刊论文
源URL[http://119.78.100.183/handle/2S10ELR8/276971]  
专题药理学第一研究室
中科院受体结构与功能重点实验室
新药研究国家重点实验室
通讯作者Xie, Hua
作者单位1.Tongji Univ, Sch Life Sci & Technol, Shanghai 200092, Peoples R China;
2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 200031, Peoples R China
推荐引用方式
GB/T 7714
Liu, Li-Ping,Han, Kun,Chen, Wei,et al. Topoisomerase II inhibitors from the roots of Stellera chamaejasme L.[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2014,22(15):4198-4203.
APA Liu, Li-Ping.,Han, Kun.,Chen, Wei.,Zhang, Ying-Ying.,Tong, Lin-Jiang.,...&Wang, Hong-Bing.(2014).Topoisomerase II inhibitors from the roots of Stellera chamaejasme L..BIOORGANIC & MEDICINAL CHEMISTRY,22(15),4198-4203.
MLA Liu, Li-Ping,et al."Topoisomerase II inhibitors from the roots of Stellera chamaejasme L.".BIOORGANIC & MEDICINAL CHEMISTRY 22.15(2014):4198-4203.
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