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BPN, a marine-derived PTP1B inhibitor, activates insulin signaling and improves insulin resistance in C2C12 myotubes

文献类型：期刊论文

作者Xu, Qi1,2,3; Luo, Jiao1,2,3; Wu, Ning1,3; Zhang, Renshuai1,3; Shi, Dayong1,2,3
刊名INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
出版日期2018
卷号106页码:379-386
关键词Bpn Protein Tyrosine Phosphatase 1b Insulin Signaling Insulin Resistance C2c12 Myotubes
ISSN号0141-8130
DOI10.1016/j.ijbiomac.2017.08.042
文献子类Article
英文摘要Insulin resistance is a key feature of type 2 diabetes mellitus (T2DM) and is characterized by defects in insulin signaling. Protein tyrosine phosphatase 1B (PTP1B) is a major negative regulator of insulin signaling cascade and has attracted intensive investigation in recent T2DM therapy study. BPN, a marine derived bromophenol compound, was isolated from the red alga Rhodomela confervoides. This study investigated the effects of BPN on the insulin signaling pathway in insulin-resistant C2C12 myotubes by inhibiting PTP1B. Molecular docking study and analysis of small-molecule interaction with PTP1B all showed BPN inhibited PTP1B activity via binding to the catalytic site through hydrogen bonds. We then found that BPN permeated into C2C12 myotubes, on the one hand, activated insulin signaling in an insulin independent manner in C2C12 cells; on the other hand, ameliorated palmitate-induced insulin resistance through augmenting insulin sensitivity. Moreover, our studies also showed that FTP1B inhibition by BPN increased glucose uptake in normal and insulin-resistant C2C12 myotubes through glucose transporter 4 (GLUT4) translocation. Taken together, BPN activates insulin signaling and alleviates insulin resistance and represents a potential candidate for further development as an antidiabetic agent. (C) 2017 Elsevier B.V. All rights reserved.
WOS关键词TYROSINE-PHOSPHATASE 1B ; GLUCOSE TRANSPORTERS ; OBESITY ; BROMOPHENOLS ; DERIVATIVES ; EXPRESSION ; DESIGN ; CANCER ; CELLS ; RATS
WOS研究方向Biochemistry & Molecular Biology ; Chemistry ; Polymer Science
语种英语
WOS记录号WOS:000417661600043
出版者ELSEVIER SCIENCE BV
资助机构National Natural Science Foundation of China(41506169) ; Key research and development project of Shandong province(2015GSF115029 ; 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 Research Centers(U1606403) ; Scientific and Technological Innovation Project - Qingdao National Laboratory for Marine Science and Technology(2015ASKJ02) ; National Program for Support of Top-notch Young Professionals ; Taishan scholar Youth Project of Shandong province ; Aoshan Talents Program - Qingdao National Laboratory for Marine Science and Technology(2015ASTP) ; 2016ZDJS07A13 ; 2016GSF115002 ; 2016GSF201193)
源URL[http://ir.qibebt.ac.cn/handle/337004/10519]  
专题中国科学院青岛生物能源与过程研究所
通讯作者Shi, Dayong
作者单位1.Chinese Acad Sci, Key Lab Expt Marine Biol, Inst Oceanol, Qingdao, Peoples R China
2.Univ Chinese Acad Sci, Beijing, Peoples R China
3.Qingdao Natl Lab Marine Sci & Technol, Lab Marine Drugs & Bioprod, Qingdao, Peoples R China
推荐引用方式
GB/T 7714		 Xu, Qi,Luo, Jiao,Wu, Ning,et al. BPN, a marine-derived PTP1B inhibitor, activates insulin signaling and improves insulin resistance in C2C12 myotubes[J]. INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,2018,106:379-386.
APA Xu, Qi,Luo, Jiao,Wu, Ning,Zhang, Renshuai,&Shi, Dayong.(2018).BPN, a marine-derived PTP1B inhibitor, activates insulin signaling and improves insulin resistance in C2C12 myotubes.INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,106,379-386.
MLA Xu, Qi,et al."BPN, a marine-derived PTP1B inhibitor, activates insulin signaling and improves insulin resistance in C2C12 myotubes".INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES 106(2018):379-386.

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来源：青岛生物能源与过程研究所

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