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![]() |
刊名 | FITOTERAPIA
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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 |
DOI | 10.1016/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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