Discovery of Novel Bromophenol Hybrids as Potential Anticancer Agents through the Ros-Mediated Apoptotic Pathway: Design, Synthesis and Biological Evaluation

doi:10.3390/md15110343

CORC > 海洋研究所 > 中国科学院海洋研究所 > 实验海洋生物学重点实验室

	Discovery of Novel Bromophenol Hybrids as Potential Anticancer Agents through the Ros-Mediated Apoptotic Pathway: Design, Synthesis and Biological Evaluation
	Wang, Li-Jun 1,2; Guo, Chuan-Long 1,2,3; Li, Xiang-Qian 1,2; Wang, Shuai-Yu 1,2; Jiang, Bo 1,2; Zhao, Yue 1,2; Luo, Jiao 1,2,3; Xu, Kuo 1,2; Liu, Hua 1,2,3; Guo, Shu-Ju 1,2
刊名	MARINE DRUGS
	2017-11-01
卷号	15 期号:11 页码:18
关键词	bromophenol hybrids anticancer structure-activity relationships ROS apoptotic pathway
ISSN号	1660-3397
DOI	10.3390/md15110343
通讯作者	Shi, Da-Yong(shidayong@qdio.ac.cn)
英文摘要	A series of bromophenol hybrids with N-containing heterocyclic moieties were designed, and their anticancer activities against a panel of five human cancer cell lines (A549, Bel7402, HepG2, HCT116 and Caco2) using MTT assay in vitro were explored. Among them, thirteen compounds (17a, 17b, 18a, 19a, 19b, 20a, 20b, 21a, 21b, 22a, 22b, 23a, and 23b) exhibited significant inhibitory activity against the tested cancer cell lines. The structure-activity relationships (SARs) of bromophenol derivatives were discussed. The promising candidate compound 17a could induce cell cycle arrest at G0/G1 phase and induce apoptosis in A549 cells, as well as caused DNA fragmentations, morphological changes and ROS generation by the mechanism studies. Furthermore, compound 17a suppression of Bcl-2 levels (decrease in the expression of the anti-apoptotic proteins Bcl-2 and down-regulation in the expression levels of Bcl-2) in A549 cells were observed, along with activation caspase-3 and PARP, which indicated that compound 17a induced A549 cells apoptosis in vitro through the ROS-mediated apoptotic pathway. These results might be useful for bromophenol derivatives to be explored and developed as novel anticancer drugs.
资助项目	National Natural Science Foundation of China[81773586] ; National Natural Science Foundation of China[81703354] ; Key research and development project of Shandong province[2016GSF201193] ; Key research and development project of Shandong province[2016ZDJS07A13] ; Key research and development project of Shandong province[2016GSF115002] ; Key research and development project of Shandong province[2016GSF115009] ; Key Research Program of Frontier Sciences, CAS[QYZDB-SSW-DQC014] ; Project of Discovery, Evaluation and Transformation of Active Natural Compounds, Strategic Biological Resources Service Network Programme of Chinese Academy of Sciences[ZSTH-026] ; NSFC-Shandong Joint Fund for Marine Science Rearch Centers[U1606403] ; Scientific and Technological Innovation Project - Qingdao National Laboratory for Marine Science and Technology[2015ASKJ02] ; Aoshan Talents Program - Qingdao National Laboratory for Marine Science and Technology[2015ASTP] ; National Program for Support of Top-notch Young Professionals ; Taishan scholar Youth Project of Shandong province
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	MDPI AG
WOS记录号	WOS:000416600200014
内容类型	期刊论文
源URL	[http://ir.qdio.ac.cn/handle/337002/157293]
专题	海洋研究所_实验海洋生物学重点实验室
通讯作者	Shi, Da-Yong
作者单位	1.Chinese Acad Sci, Inst Oceanol, Key Lab Expt Marine Biol, Qingdao 266071, Shandong, Peoples R China 2.Qingdao Natl Lab Marine Sci & Technol, Lab Marine Drugs & Bioprod, Qingdao 266071, Shandong, Peoples R China 3.Univ Chinese Acad Sci, Beijing 10049, Peoples R China
推荐引用方式 GB/T 7714	Wang, Li-Jun,Guo, Chuan-Long,Li, Xiang-Qian,et al. Discovery of Novel Bromophenol Hybrids as Potential Anticancer Agents through the Ros-Mediated Apoptotic Pathway: Design, Synthesis and Biological Evaluation[J]. MARINE DRUGS,2017,15(11):18.
APA	Wang, Li-Jun.,Guo, Chuan-Long.,Li, Xiang-Qian.,Wang, Shuai-Yu.,Jiang, Bo.,...&Shi, Da-Yong.(2017).Discovery of Novel Bromophenol Hybrids as Potential Anticancer Agents through the Ros-Mediated Apoptotic Pathway: Design, Synthesis and Biological Evaluation.MARINE DRUGS,15(11),18.
MLA	Wang, Li-Jun,et al."Discovery of Novel Bromophenol Hybrids as Potential Anticancer Agents through the Ros-Mediated Apoptotic Pathway: Design, Synthesis and Biological Evaluation".MARINE DRUGS 15.11(2017):18.