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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 | |
| Source Publication | RSC ADVANCES
 |
| Volume | 10Issue:6Pages:3429-3437 |
| Corresponding Author | Jiang, Bo(jiangbo@qdio.ac.cn) |
| Abstract | 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. |
| DOI | 10.1039/c9ra10660j |
| Indexed By | SCI |
| Language | 英语 |
| Funding Project | Key Research and Development Project of Shandong province[2018GSF118208] ; Key Research and Development Project of Shandong province[2018GSF118223] ; NSFC-Shandong Joint Fund[U1706213] |
| WOS Research Area | Chemistry |
| WOS Subject | Chemistry, Multidisciplinary |
| WOS ID | WOS:000508849900044 |
| Publisher | ROYAL SOC CHEMISTRY |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.qdio.ac.cn/handle/337002/164470 |
| Collection | 实验海洋生物学重点实验室 |
| Corresponding Author | Jiang, Bo |
| Affiliation | 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 |
| First Author Affilication | Institute of Oceanology, Chinese Academy of Sciences |
| Corresponding Author Affilication | Institute of Oceanology, Chinese Academy of Sciences |
| Recommended Citation 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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