中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
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
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
DOI10.1038/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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