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A Novel Bromophenol Derivative BOS-102 Induces Cell Cycle Arrest and Apoptosis in Human A549 Lung Cancer Cells via ROS-Mediated PI3K/Akt and the MAPK Signaling Pathway
Guo, Chuan-Long1,2,3; Wang, Li-Jun1,2; Zhao, Yue1,2; Liu, Hua1,2,3; Li, Xiang-Qian1,2; Jiang, Bo1,2; Luo, Jiao1,2,3; Guo, Shu-Ju1,2; Wu, Ning1,2; Shi, Da-Yong1,2,3
2018-02-01
Source PublicationMARINE DRUGS
ISSN1660-3397
Volume16Issue:2Pages:13
Corresponding AuthorShi, Da-Yong(shidayong@qdio.ac.cn)
AbstractBromophenol is a type of natural marine product. It has excellent biological activities, especially anticancer activities. In our study of searching for potent anticancer drugs, a novel bromophenol derivative containing indolin-2-one moiety, 3-(4-(3-([1,4-bipiperidin]-1-yl)propoxy)-3-bromo-5-methoxybenzylidene)-N-(4-bromophenyl)-2-oxoindoline-5-sulfonamide (BOS-102) was synthesized, which showed excellent anticancer activities on human lung cancer cell lines. A study of the mechanisms indicated that BOS-102 could significantly block cell proliferation in human A549 lung cancer cells and effectively induce G0/G1 cell cycle arrest via targeting cyclin D1 and cyclin-dependent kinase 4 (CDK4). BOS-102 could also induce apoptosis, including activating caspase-3 and poly (ADP-ribose) polymerase (PARP), increasing the Bax/Bcl-2 ratio, enhancing reactive oxygen species (ROS) generation, decreasing mitochondrial membrane potential (MMP, (m)), and leading cytochrome c release from mitochondria. Further research revealed that BOS-102 deactivated the PI3K/Akt pathway and activated the mitogen-activated protein kinase (MAPK) signaling pathway resulting in apoptosis and cell cycle arrest, which indicated that BOS-102 has the potential to develop into an anticancer drug.
Keywordbromophenol molecular mechanisms apoptosis cell cycle PI3K Akt p38 ERK ROS human lung cancer
DOI10.3390/md16020043
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 the Support of Top-notch Young Professionals ; Taishan scholar Youth Project of Shandong province
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000427528800005
PublisherMDPI
Citation statistics
Document Type期刊论文
Identifierhttp://ir.qdio.ac.cn/handle/337002/158426
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, Peoples R China
2.Qingdao Natl Lab Marine Sci & Technol, Lab Marine Drugs & Bioprod, Qingdao 266071, Peoples R China
3.Univ Chinese Acad Sci, Beijing 10049, Peoples R China
First Author AffilicationKey Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences
Corresponding Author AffilicationKey Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences
Recommended Citation
GB/T 7714
Guo, Chuan-Long,Wang, Li-Jun,Zhao, Yue,et al. A Novel Bromophenol Derivative BOS-102 Induces Cell Cycle Arrest and Apoptosis in Human A549 Lung Cancer Cells via ROS-Mediated PI3K/Akt and the MAPK Signaling Pathway[J]. MARINE DRUGS,2018,16(2):13.
APA Guo, Chuan-Long.,Wang, Li-Jun.,Zhao, Yue.,Liu, Hua.,Li, Xiang-Qian.,...&Shi, Da-Yong.(2018).A Novel Bromophenol Derivative BOS-102 Induces Cell Cycle Arrest and Apoptosis in Human A549 Lung Cancer Cells via ROS-Mediated PI3K/Akt and the MAPK Signaling Pathway.MARINE DRUGS,16(2),13.
MLA Guo, Chuan-Long,et al."A Novel Bromophenol Derivative BOS-102 Induces Cell Cycle Arrest and Apoptosis in Human A549 Lung Cancer Cells via ROS-Mediated PI3K/Akt and the MAPK Signaling Pathway".MARINE DRUGS 16.2(2018):13.
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