中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
New cytotoxic 19-norbufadienolide and bufogargarizin isolated from Chan Su

文献类型:期刊论文

作者Chen, Hu2; Meng, Yu-Hui1; Guo, De-An1; Liu, Xuan1; Liu, Jun-Hua1; Hu, Li-Hong1,2
刊名FITOTERAPIA
出版日期2015-07
卷号104页码:1-6
关键词Toad venom Bufo gargarizans Cantor Bufadienolide Cytotoxicity
ISSN号0367-326X
DOI10.1016/j.fitote.2015.05.011
文献子类Article
英文摘要One new 19-norbufadienolide (1) and one new bufogargarizin (2), together with twelve known bufadienolides (3-14, resp.) were isolated from Chan Su, a traditional Chinese medicine that is used in the treatment of cancer. Their structures were elucidated on the basis of detailed spectroscopic analysis and comparison of corresponding data that is previously reported. The cytotoxic activities of the isolated compounds were evaluated on HeLa and A549 cell lines. Though 1 and 2 showed weak cytotoxic activities on both cell lines, compounds 4 and 5 showed lower IC50 values than bufalin, the most widely studied bufadienolide in Chan Su. Furthermore, four 3-ester derivatives (15-18) of compound 4 were synthesized and their cytotoxic activities were also evaluated. Analysis of the structure-activity relationship indicated that bufadienolides with aldehyde group at C-10 or alpha-hydroxyl group at C-11 exhibit stronger cytotoxic activities on both cell lines. The cytotoxic activity of arenobufagin-3-ester derivative 17 was 4-fold higher than compound 4. (C) 2015 Elsevier B.V. All rights reserved.
WOS关键词BUFO-BUFO-GARGARIZANS ; C-23 STEROIDS ; BUFADIENOLIDES ; VENOM ; BUFALIN ; CELLS ; CINOBUFOTALIN ; CINOBUFAGIN ; INHIBITION ; APOPTOSIS
资助项目National Science Foundation of China[81273397] ; National Science Foundation of China[81402811] ; Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2013ZX09508104] ; Chinese National Science & Technology Major Project "Key New Drug Creation and Manufacturing Program"[2014ZX09301306-003] ; Chinese Postdoctoral Science Foundation[2014M550255]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000357547100001
出版者ELSEVIER SCIENCE BV
源URL[http://119.78.100.183/handle/2S10ELR8/276482]  
专题上海中药现代化研究中心
通讯作者Liu, Jun-Hua
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Res Ctr Modernizat Tradit Chinese Med, Shanghai 201203, Peoples R China
2.E China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China;
推荐引用方式
GB/T 7714
Chen, Hu,Meng, Yu-Hui,Guo, De-An,et al. New cytotoxic 19-norbufadienolide and bufogargarizin isolated from Chan Su[J]. FITOTERAPIA,2015,104:1-6.
APA Chen, Hu,Meng, Yu-Hui,Guo, De-An,Liu, Xuan,Liu, Jun-Hua,&Hu, Li-Hong.(2015).New cytotoxic 19-norbufadienolide and bufogargarizin isolated from Chan Su.FITOTERAPIA,104,1-6.
MLA Chen, Hu,et al."New cytotoxic 19-norbufadienolide and bufogargarizin isolated from Chan Su".FITOTERAPIA 104(2015):1-6.

入库方式: OAI收割

来源:上海药物研究所

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