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Discovery of Novel Bromophenol Hybrids as Potential Anticancer Agents through the Ros-Mediated Apoptotic Pathway: Design, Synthesis and Biological Evaluation
Wang, Li-Jun1,2; Guo, Chuan-Long1,2,3; Li, Xiang-Qian1,2; Wang, Shuai-Yu1,2; Jiang, Bo1,2; Zhao, Yue1,2; Luo, Jiao1,2,3; Xu, Kuo1,2; Liu, Hua1,2,3; Guo, Shu-Ju1,2; Wu, Ning1,2; Shi, Da-Yong1,2,3
2017-11-01
Source PublicationMARINE DRUGS
ISSN1660-3397
Volume15Issue:11Pages:18
Corresponding AuthorShi, Da-Yong(shidayong@qdio.ac.cn)
AbstractA 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.
Keywordbromophenol hybrids anticancer structure-activity relationships ROS apoptotic pathway
DOI10.3390/md15110343
Indexed BySCI
Language英语
Funding ProjectNational 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 Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000416600200014
PublisherMDPI AG
Citation statistics
Document Type期刊论文
Identifierhttp://ir.qdio.ac.cn/handle/337002/157294
Collection实验海洋生物学重点实验室
Corresponding AuthorShi, Da-Yong
Affiliation1.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
First Author AffilicationInstitute of Oceanology, Chinese Academy of Sciences
Corresponding Author AffilicationInstitute of Oceanology, Chinese Academy of Sciences
Recommended Citation
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.
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