Novel microtubule-targeted agent 6-chloro-4-(methoxyphenyl) coumarin induces G(2)-M arrest and apoptosis in HeLa cells
文献类型：期刊论文
| 作者 | Ma, Yi-ming; Zhou, Yu-bo ; Xie, Chuan-ming; Chen, Dong-mei; Li, Jia
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| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2012-03 |
| 卷号 | 33期号:3页码:407-417 |
| 关键词 | anticancer drug 6-chloro-4-(methoxyphenyl) coumarin cell cycle arrest microtubule depolymerization apoptosis |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2011.176 |
| 文献子类 | Article |
| 英文摘要 | Aim: To identify a novel coumarin analogue with the highest anticancer activity and to further investigate its anticancer mechanisms. Methods: The viability of cancer cells was investigated using the MTT assay. The cell cycle progression was evaluated using both flow cytometric and Western blotting analysis. Microtubule depolymerization was observed with immunocytochemistry in vivo and a tubulin depolymerization assay in vitro. Apoptosis was demonstrated using Annexin V/Propidium Iodide (PI) double-staining and sub-G(1) analysis. Results: Among 36 analogues of coumarin, 6-chloro-4-(methoxyphenyl) coumarin showed the best anticancer activity (IC50 value about 200 nmol/L) in HCT116 cells. The compound had a broad spectrum of anticancer activity against 9 cancer cell lines derived from colon cancer, breast cancer, liver cancer, cervical cancer, leukemia, epidermoid cancer with IC50 value of 75 nmol/L-1.57 mu mol/L but with low cytotocitity against WI-38 human lung fibroblasts (IC50 value of 12.128 mu mol/L). The compound (0.04-10 mu mol/L) induced G(2)-M phase arrest in HeLa cells in a dose-dependent manner, which was reversible after the compound was removed. The compound (10-300 mu mol/L) induced the depolymerization of purified porcine tubulin in vitro. Finally, the compound (0.04-2.5 mu mol/L) induced apoptosis of HeLa cells in dose-and time-dependent manners. Conclusion: 6-Chloro-4-(methoxyphenyl) coumarin is a novel microtubule-targeting agent that induces G(2)-M arrest and apoptosis in HeLa cells. |
| WOS关键词 | ACTIVATED PROTEIN-KINASE ; TUBULIN-BINDING AGENT ; IN-VIVO ; ANTIMICROBIAL ACTIVITY ; ANTICANCER ACTIVITY ; CYCLE ARREST ; CANCER-CELLS ; DERIVATIVES ; INHIBITOR ; RESISTANT |
| 资助项目 | National Natural Science Foundation of China[30801405] ; National Natural Science Foundation of China[81072667] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:4455257 |
| WOS记录号 | WOS:000301187300014 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278169]  |
| 专题 | 国家新药筛选中心 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 | Zhou, Yu-bo |
| 作者单位 | Chinese Acad Sci, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ma, Yi-ming,Zhou, Yu-bo,Xie, Chuan-ming,et al. Novel microtubule-targeted agent 6-chloro-4-(methoxyphenyl) coumarin induces G(2)-M arrest and apoptosis in HeLa cells[J]. ACTA PHARMACOLOGICA SINICA,2012,33(3):407-417. |
| APA | Ma, Yi-ming,Zhou, Yu-bo,Xie, Chuan-ming,Chen, Dong-mei,&Li, Jia.(2012).Novel microtubule-targeted agent 6-chloro-4-(methoxyphenyl) coumarin induces G(2)-M arrest and apoptosis in HeLa cells.ACTA PHARMACOLOGICA SINICA,33(3),407-417. |
| MLA | Ma, Yi-ming,et al."Novel microtubule-targeted agent 6-chloro-4-(methoxyphenyl) coumarin induces G(2)-M arrest and apoptosis in HeLa cells".ACTA PHARMACOLOGICA SINICA 33.3(2012):407-417. |
入库方式： OAI收割
来源：上海药物研究所
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