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BPN, a marine-derived PTP1B inhibitor, activates insulin signaling and improves insulin resistance in C2C12 myotubes
Xu, Qi1,2,3; Luo, Jiao1,2,3; Wu, Ning1,3; Zhang, Renshuai1,3; Shi, Dayong1,2,3
2018
发表期刊INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
卷号106页码:379-386
文章类型Article
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.
关键词Bpn Protein Tyrosine Phosphatase 1b Insulin Signaling Insulin Resistance C2c12 Myotubes
DOI10.1016/j.ijbiomac.2017.08.042
收录类别SCI
语种英语
WOS记录号WOS:000417661600043
引用统计
文献类型期刊论文
版本出版稿
条目标识符http://ir.qdio.ac.cn/handle/337002/154321
专题实验海洋生物学重点实验室
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
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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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