PTP1B inhibitors from the seeds of Iris sanguinea and their insulin mimetic activities via AMPK and ACC phosphorylation |
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Authors: | Jun Li Yang Thi Kim Quy Ha Ba Wool Lee Jinwoong Kim Won Keun Oh |
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Affiliation: | Korea Bioactive Natural Material Bank, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 08826, Republic of Korea |
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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. |
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Keywords: | Triterpene PTP1B AMPK Glucose uptake |
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