PTP1B inhibitors from the seeds of Iris sanguinea and their insulin mimetic activities via AMPK and ACC phosphorylation | |
Won Keun Oh2; Yang JL(杨军丽)1,2![]() | |
刊名 | Bioorganic and Medicinal Chemistry Letters
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2017 | |
卷号 | 27期号:22页码:5076-5081 |
关键词 | Iris Sanguinea Triterpene Ptp1b Ampk Glucose Uptake |
ISSN号 | 0960-894X |
DOI | 10.1016/j.bmcl.2017.09.031 |
英文摘要 | To find PTP1B inhibitors from natural products, two new compounds (1 and 2), along with nine known compounds (3-11), were isolated from a methanol-soluble extract of Iris sanguinea seeds. The structures of compounds 1 and 2 were determined based on extensive spectroscopic data analysis including UV, IR, NMR, and MS. The IC50 value of compound 5 on protein tyrosine phosphatase 1B (PTP1B) inhibitory activity is 7.30 +/- 0.88 mu M with a little activity compared to the IC50 values of the tested positive compound. Compound 5 significantly enhanced glucose uptake and activation of pACC, pAMPK and partially Erk1/2 signaling. These results suggest that compound 5 from Iris sanguinea seeds are utilized as both PTP1B inhibitors and regulators of glucose uptake. These beneficial effects could be applied to treat metabolic diseases such as diabetes and obesity. |
学科主题 | 分析化学与药物化学 |
资助项目 | 药物化学成分研究组 |
语种 | 英语 |
WOS记录号 | WOS:000414000000027 |
资助机构 | the Korea Bioactive Natural Material Bank (NRF-2012M3A9B8021570);the Bio & Technology Development (2016M3A9A5919548) of the National Research Foundation of Korea (NRF);which is funded by the Ministry of Science, ICT & Future Planning |
内容类型 | 期刊论文 |
源URL | [http://ir.licp.ac.cn/handle/362003/22766] ![]() |
专题 | 兰州化学物理研究所_中科院西北特色植物资源化学重点实验室/甘肃省天然药物重点实验室 |
通讯作者 | Won Keun Oh |
作者单位 | 1.CAS Key Laboratory of Chemistry of Northwestern Plant Resources and Key Laboratory for Natural Medicine of Gansu Province, Lanzhou Institute of Chemical Physics, Chinese Academy of Science (CAS), Lanzhou 730000, PR China 2.Korea Bioactive Natural Material Bank, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea |
推荐引用方式 GB/T 7714 | Won Keun Oh,Yang JL,Thi Kim Quy Ha,et al. PTP1B inhibitors from the seeds of Iris sanguinea and their insulin mimetic activities via AMPK and ACC phosphorylation[J]. Bioorganic and Medicinal Chemistry Letters,2017,27(22):5076-5081. |
APA | Won Keun Oh,Yang JL,Thi Kim Quy Ha,Ba Wool Lee,&Jinwoong Kim.(2017).PTP1B inhibitors from the seeds of Iris sanguinea and their insulin mimetic activities via AMPK and ACC phosphorylation.Bioorganic and Medicinal Chemistry Letters,27(22),5076-5081. |
MLA | Won Keun Oh,et al."PTP1B inhibitors from the seeds of Iris sanguinea and their insulin mimetic activities via AMPK and ACC phosphorylation".Bioorganic and Medicinal Chemistry Letters 27.22(2017):5076-5081. |
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