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| Marine bromophenol bis(2,3-dibromo-4,5-dihydroxybenzyl) ether, induces mitochondrial apoptosis in K562 cells and inhibits topoisomerase I in vitro | |
| Liu, Ming1; Zhang, Wei2; Wei, Jianteng1; Qiu, Lin3; Lin, Xiukun1; Lin, XK (reprint author), Chinese Acad Sci, Inst Oceanol, 7 Nanhai Rd, Qingdao 266071, Peoples R China. | |
| 2012-06-01 | |
| 发表期刊 | TOXICOLOGY LETTERS
 |
| ISSN | 0378-4274 |
| 卷号 | 211期号:2页码:126-134 |
| 文章类型 | Article |
| 摘要 | Bis(2,3-dibromo-4,5-dihydroxybenzyl) ether (BDDE) is a marine bromophenol compound derived from marine algae. Previous reports have shown that BDDE possesses cytotoxic activity. However, the mechanisms of its apoptotic activity as well as its potential cellular targets remain unclear. The present study demonstrated that BDDE displays broad-spectrum in vitro anticancer capabilities and exhibits potent apoptotic activity in K562 cells via mitochondrial pathway. Further study revealed that BDDE inhibits the activity of topoisomerase I but does not stimulate the formation of topoisomerase I-DNA complex nor intercalate into DNA. Ethidium bromide displacement fluorescence assay and molecular modeling results showed that BDDE mainly targets DNA and binds to DNA minor groove, and thereafter inhibits the activity of topoisomerase I. The results of this study indicated that BDDE, which has unique chemical structure different from current topoisomerase I inhibitors, could serve as a lead template for rational drug design and for future anticancer agents development. (C) 2012 Elsevier Ireland Ltd. All rights reserved. |
| 关键词 | Apoptosis Bis(2 Topoisomerase i Inhibition 3-dibromo-4 Minor Groove Binding 5-dihydroxybenzyl) Ether |
| 学科领域 | Toxicology |
| DOI | 10.1016/j.toxlet.2012.03.771 |
| URL | 查看原文 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000304744700006 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.qdio.ac.cn/handle/337002/12359 |
| 专题 | 实验海洋生物学重点实验室 |
| 通讯作者 | Lin, XK (reprint author), Chinese Acad Sci, Inst Oceanol, 7 Nanhai Rd, Qingdao 266071, Peoples R China. |
| 作者单位 | 1.Chinese Acad Sci, Inst Oceanol, Qingdao 266071, Peoples R China 2.So Res Inst, Birmingham, AL 35205 USA 3.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Nutr Sci, Shanghai 200031, Peoples R China |
| 第一作者单位 | 中国科学院海洋研究所 |
| 推荐引用方式 GB/T 7714 | Liu, Ming,Zhang, Wei,Wei, Jianteng,et al. Marine bromophenol bis(2,3-dibromo-4,5-dihydroxybenzyl) ether, induces mitochondrial apoptosis in K562 cells and inhibits topoisomerase I in vitro[J]. TOXICOLOGY LETTERS,2012,211(2):126-134. |
| APA | Liu, Ming,Zhang, Wei,Wei, Jianteng,Qiu, Lin,Lin, Xiukun,&Lin, XK .(2012).Marine bromophenol bis(2,3-dibromo-4,5-dihydroxybenzyl) ether, induces mitochondrial apoptosis in K562 cells and inhibits topoisomerase I in vitro.TOXICOLOGY LETTERS,211(2),126-134. |
| MLA | Liu, Ming,et al."Marine bromophenol bis(2,3-dibromo-4,5-dihydroxybenzyl) ether, induces mitochondrial apoptosis in K562 cells and inhibits topoisomerase I in vitro".TOXICOLOGY LETTERS 211.2(2012):126-134. |
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