PTP1B inhibitors from the seeds of Iris sanguinea and their insulin mimetic activities via AMPK and ACC phosphorylation | |
Department | 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 |
Yang JL(杨军丽)1,2; Thi Kim Quy Ha1; Ba Wool Lee1; Jinwoong Kim1; Won Keun Oh1 | |
2017 | |
Source Publication | Bioorganic and Medicinal Chemistry Letters |
ISSN | 0960-894X |
Volume | 27Issue:22Pages:5076-5081 |
Abstract | 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. |
Keyword | Iris Sanguinea Triterpene Ptp1b Ampk Glucose Uptake |
Subject Area | 分析化学与药物化学 |
DOI | 10.1016/j.bmcl.2017.09.031 |
Funding Organization | 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 |
Indexed By | SCI |
If | 2.454 |
Language | 英语 |
Funding Project | 药物化学成分研究组 |
compositor | 第二作者单位 |
Citation statistics | |
Document Type | 期刊论文 |
Identifier | http://ir.licp.cn/handle/362003/22766 |
Collection | 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 |
Corresponding Author | Won Keun Oh |
Affiliation | 1.Korea Bioactive Natural Material Bank, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea 2.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 |
Recommended Citation GB/T 7714 | Yang JL,Thi Kim Quy Ha,Ba Wool Lee,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 | Yang JL,Thi Kim Quy Ha,Ba Wool Lee,Jinwoong Kim,&Won Keun Oh.(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 | Yang JL,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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