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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
发表期刊MARINE DRUGS
ISSN1660-3397
卷号16期号:2页码:13
通讯作者Shi, Da-Yong(shidayong@qdio.ac.cn)
摘要Bromophenol 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.
关键词bromophenol molecular mechanisms apoptosis cell cycle PI3K Akt p38 ERK ROS human lung cancer
DOI10.3390/md16020043
收录类别SCI
语种英语
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 the Support of Top-notch Young Professionals ; Taishan scholar Youth Project of Shandong province ; 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 the Support of Top-notch Young Professionals ; Taishan scholar Youth Project of Shandong province
WOS研究方向Pharmacology & Pharmacy
WOS类目Chemistry, Medicinal
WOS记录号WOS:000427528800005
出版者MDPI
引用统计
被引频次:39[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.qdio.ac.cn/handle/337002/158426
专题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, 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
第一作者单位实验海洋生物学重点实验室
通讯作者单位实验海洋生物学重点实验室
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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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