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A novel fluorinated thiosemicarbazone derivative-2-(3,4-difluorobenzylidene) hydrazinecarbothioamide induces apoptosis in human A549 lung cancer cells via ROS-mediated mitochondria-dependent pathway
Zhao, Yue1,2,3; Guo, Chuanlong2,3,4; Wang, Lijun2,3; Wang, Shuaiyu2,3; Li, Xiangqian2,3; Jiang, Bo2,3; Wu, Ning2,3; Guo, Shuju2,3; Zhang, Renshuai2,3; Liu, Kun1; Shi, Dayong2,3,4
2017-09-09
发表期刊BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
卷号491期号:1页码:65-71
文章类型Article
摘要Thiosemicarbazone, a class of compounds with excellent biological activity, especially antitumor activity, have attracted wide attention. In this study, a novel fluorinated thiosemicarbazone derivative, 2-(3,4difluorobenzylidene) hydrazinecarbothioamide (compound 1) was synthesized and its antitumor activities were further investigated on a non-small cell lung cancer cell line (A549) along with its underlying mechanisms. Compound 1 showed significant anti-proliferative activity on A549 cells, which was further proved by colony formation experiment. Compound 1 also inhibits the invasion of A549 cells in a trans-well culture system. Moreover, compound 1 markedly induced apoptosis on A549 cells, and the ratio of Bcl-2/Bax was decreased while the amount of p53, Cleaved-Caspase 3 and Cleaved-PARP expression were increased significantly. Compound 1 decreased the mitochondrial membrane potential, while the content of reactive oxygen was increased obviously. It is revealed that compound 1 mediated cell cycle arrest in GO/G1 phase by reducing G1 phase dependent proteins, CDK4 and Cyclin Dl. As a result, it is indicated that compound 1 induced apoptosis on A549 cells was realized by regulating ROS-mediated mitochondria-dependent signaling pathway. (C) 2017 Elsevier Inc. All rights reserved.
关键词Thiosemicarbazone Anticancer 2-(3 Apoptosis 4-difluorobenzylidene) Hydrazinecarbothioamide Ros Mitochondria-dependent Pathway
DOI10.1016/j.bbrc.2017.07.042
收录类别SCI
语种英语
WOS记录号WOS:000408518700011
引用统计
文献类型期刊论文
版本出版稿
条目标识符http://ir.qdio.ac.cn/handle/337002/143157
专题海洋生物技术研发中心
作者单位1.Qingdao Univ, Sch Pharm, Dept Pharmaceut Anal, Qingdao 266021, Peoples R China
2.Chinese Acad Sci, Inst Oceanol, Key Lab Expt Marine Biol, Qingdao 266071, Peoples R China
3.Qingdao Natl Lab Marine Sci & Technol, Lab Marine Drugs & Bioprod, Qingdao 266071, Peoples R China
4.Univ Chinese Acad Sci, Beijing, Peoples R China
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Zhao, Yue,Guo, Chuanlong,Wang, Lijun,et al. A novel fluorinated thiosemicarbazone derivative-2-(3,4-difluorobenzylidene) hydrazinecarbothioamide induces apoptosis in human A549 lung cancer cells via ROS-mediated mitochondria-dependent pathway[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,2017,491(1):65-71.
APA Zhao, Yue.,Guo, Chuanlong.,Wang, Lijun.,Wang, Shuaiyu.,Li, Xiangqian.,...&Shi, Dayong.(2017).A novel fluorinated thiosemicarbazone derivative-2-(3,4-difluorobenzylidene) hydrazinecarbothioamide induces apoptosis in human A549 lung cancer cells via ROS-mediated mitochondria-dependent pathway.BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,491(1),65-71.
MLA Zhao, Yue,et al."A novel fluorinated thiosemicarbazone derivative-2-(3,4-difluorobenzylidene) hydrazinecarbothioamide induces apoptosis in human A549 lung cancer cells via ROS-mediated mitochondria-dependent pathway".BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS 491.1(2017):65-71.
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