Back to Search Start Over

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

Authors :
Yang, Jun Li
Ha, Thi Kim Quy
Lee, Ba Wool
Kim, Jinwoong
Oh, Won Keun
Source :
Bioorganic & Medicinal Chemistry Letters. Nov2017, Vol. 27 Issue 22, p5076-5081. 6p.
Publication Year :
2017

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 IC 50 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 IC 50 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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
0960894X
Volume :
27
Issue :
22
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
125922535
Full Text :
https://doi.org/10.1016/j.bmcl.2017.09.031