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 PublicationBioorganic and Medicinal Chemistry Letters
ISSN0960-894X
Volume27Issue: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.

KeywordIris Sanguinea Triterpene Ptp1b Ampk Glucose Uptake
Subject Area分析化学与药物化学
DOI10.1016/j.bmcl.2017.09.031
Funding Organizationthe 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 BySCI
If2.454
Language英语
Funding Project药物化学成分研究组
compositor第二作者单位
Citation statistics
Cited Times:20[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://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 AuthorWon Keun Oh
Affiliation1.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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