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PTP1B inhibitors from the seeds of Iris sanguinea and their insulin mimetic activities via AMPK and ACC phosphorylation

Cited 20 time in Web of Science Cited 22 time in Scopus
Authors

Yang, Jun Li; Ha, Thi Kim Quy; Lee, Ba Wool; Kim, Jinwoong; Oh, Won Keun

Issue Date
2017-11
Publisher
Pergamon Press Ltd.
Citation
Bioorganic and Medicinal Chemistry Letters, Vol.27 No.22, pp.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 µM 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.
ISSN
0960-894X
Language
English
URI
https://hdl.handle.net/10371/148288
DOI
https://doi.org/10.1016/j.bmcl.2017.09.031
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