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
文献类型:期刊论文
作者 | Guo, Shuju2,3,4; Wang, Lijun2,3,4; Chen, Dong1; Jiang, Bo2,3,4 |
刊名 | RSC ADVANCES
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出版日期 | 2020-01-20 |
卷号 | 10期号:6页码:3429-3437 |
DOI | 10.1039/c9ra10660j |
通讯作者 | Jiang, Bo(jiangbo@qdio.ac.cn) |
英文摘要 | 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. |
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] |
WOS研究方向 | Chemistry |
语种 | 英语 |
WOS记录号 | WOS:000508849900044 |
出版者 | ROYAL SOC CHEMISTRY |
源URL | [http://ir.qdio.ac.cn/handle/337002/164469] ![]() |
专题 | 海洋研究所_实验海洋生物学重点实验室 |
通讯作者 | Jiang, Bo |
作者单位 | 1.Ocean Univ China, Sch Med & Pharm, Key Lab Marine Drugs, Chinese Minist Educ, Yushan Rd, Qingdao 266003, Peoples R China 2.Chinese Acad Sci, Inst Oceanol, Key Lab Expt Marine Biol, 7 Nanhai Rd, Qingdao 266071, Peoples R China 3.Chinese Acad Sci, Ctr Ocean Megasci, 7 Nanhai Rd, Qingdao 266071, Peoples R China 4.Qingdao Natl Lab Marine Sci & Technol, Lab Marine Drugs & Bioprod, Qingdao, Peoples R China |
推荐引用方式 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. |
入库方式: OAI收割
来源:海洋研究所
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