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Effects of a natural PTP1B inhibitor from Rhodomela confervoides on the amelioration of fatty acid-induced insulin resistance in hepatocytes and hyperglycaemia in STZ-induced diabetic rats
Guo, Shuju1,2,3; Wang, Lijun1,2,3; Chen, Dong4; Jiang, Bo1,2,3
2020-01-20
发表期刊RSC ADVANCES
卷号10期号:6页码:3429-3437
通讯作者Jiang, Bo(jiangbo@qdio.ac.cn)
摘要PTP1B is a key negative regulator of insulin signaling transduction, and the inhibition of PTP1B has emerged as a potential therapeutic strategy to treat T2DM. 3,4-Dibromo-5-(2-bromo-6-(ethoxymethyl)-3,4-dihydroxybenzyl)benzene-1,2-diol (BPN), a natural bromophenol isolated from marine red alga Rhodomela confervoides, was found to inhibit PTP1B activity in our previous study. Herein, we identified that BPN functioned as a competitive PTP1B inhibitor and enhanced phosphorylation of IR beta, IRS-1 and Akt in palmitate acid-induced insulin-resistant HepG2 cells. Moreover, 2-deoxyglucose uptake technology-based characterization demonstrated that BPN could stimulate glucose uptake in HepG2 cells. Furthermore, the effects of BPN against oxidative stress were investigated and showed that BPN attenuated oxidative stress by attenuating ROS generation. Finally, long-term oral administration of BPN at dose of 20 mg kg(-1) significantly reduced blood glucose levels in streptozotocin-induced diabetic mice and no visible toxic effects were observed. Our work is thus expected to provide a natural uncharged PTP1B inhibitor that could be used as a potential lead compound for further research.
DOI10.1039/c9ra10660j
收录类别SCI
语种英语
资助项目Key Research and Development Project of Shandong province[2018GSF118208] ; Key research and development project of Shandong province[2018GSF118223] ; NSFC-Shandong Joint Fund[U1706213] ; Key Research and Development Project of Shandong province[2018GSF118208] ; Key Research and Development Project of Shandong province[2018GSF118223] ; NSFC-Shandong Joint Fund[U1706213]
WOS研究方向Chemistry
WOS类目Chemistry, Multidisciplinary
WOS记录号WOS:000508849900044
出版者ROYAL SOC CHEMISTRY
引用统计
被引频次:4[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/337002/164470
专题实验海洋生物学重点实验室
通讯作者Jiang, Bo
作者单位1.Chinese Acad Sci, Inst Oceanol, Key Lab Expt Marine Biol, 7 Nanhai Rd, Qingdao 266071, Peoples R China
2.Chinese Acad Sci, Ctr Ocean Megasci, 7 Nanhai Rd, Qingdao 266071, Peoples R China
3.Qingdao Natl Lab Marine Sci & Technol, Lab Marine Drugs & Bioprod, Qingdao, Peoples R China
4.Ocean Univ China, Sch Med & Pharm, Key Lab Marine Drugs, Chinese Minist Educ, Yushan Rd, Qingdao 266003, Peoples R China
第一作者单位中国科学院海洋研究所;  中国科学院海洋大科学研究中心
通讯作者单位中国科学院海洋研究所;  中国科学院海洋大科学研究中心
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GB/T 7714
Guo, Shuju,Wang, Lijun,Chen, Dong,et al. Effects of a natural PTP1B inhibitor from Rhodomela confervoides on the amelioration of fatty acid-induced insulin resistance in hepatocytes and hyperglycaemia in STZ-induced diabetic rats[J]. RSC ADVANCES,2020,10(6):3429-3437.
APA Guo, Shuju,Wang, Lijun,Chen, Dong,&Jiang, Bo.(2020).Effects of a natural PTP1B inhibitor from Rhodomela confervoides on the amelioration of fatty acid-induced insulin resistance in hepatocytes and hyperglycaemia in STZ-induced diabetic rats.RSC ADVANCES,10(6),3429-3437.
MLA Guo, Shuju,et al."Effects of a natural PTP1B inhibitor from Rhodomela confervoides on the amelioration of fatty acid-induced insulin resistance in hepatocytes and hyperglycaemia in STZ-induced diabetic rats".RSC ADVANCES 10.6(2020):3429-3437.
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