Institutional Repository of Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences
| 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 Publication | MARINE DRUGS
 |
| ISSN | 1660-3397 |
| Volume | 16Issue:2Pages:13 |
| Corresponding Author | Shi, Da-Yong(shidayong@qdio.ac.cn) |
| Abstract | 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. |
| Keyword | bromophenol molecular mechanisms apoptosis cell cycle PI3K Akt p38 ERK ROS human lung cancer |
| DOI | 10.3390/md16020043 |
| Indexed By | SCI |
| Language | 英语 |
| Funding Project | 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 Research Area | Pharmacology & Pharmacy |
| WOS Subject | Chemistry, Medicinal |
| WOS ID | WOS:000427528800005 |
| Publisher | MDPI |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.qdio.ac.cn/handle/337002/158426 |
| Collection | 实验海洋生物学重点实验室 |
| Corresponding Author | Shi, Da-Yong |
| Affiliation | 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 |
| First Author Affilication | Key Laboratory of Experimental Marine Biology, Institute of Oceanology, Chinese Academy of Sciences |
| Corresponding Author Affilication | Key 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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| File Name/Size | DocType | Version | Access | License | ||
| A Novel Bromophenol （5208KB） | 期刊论文 | 出版稿 | 开放获取 | CC BY-NC-SA | View Application Full Text | |
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