期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 2, 页码 318-321出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.12.021
关键词
Flemingia philippinensis; Chromenedione derivatives; Protein tyrosine phosphatase 1B (PTP1B); Philippin A, B, C
资金
- Next-Generation BioGreen 21 program (SSAC) [PJ01107001]
- Ministry of Education, South Korea [2015R1A6A1A03031413]
- BK21 plus program
- Scientific Research Foundation for the Returned Overseas Chinese Scholars, State Education Ministry and Program for Young Teachers Scientific Research in Qiqihar University [2014k-M27]
Protein tyrosine phosphatase 1B (PTP1B) is an important target to treat obesity and diabetes due to its key roles in insulin and leptin signaling. The MeOH extracts of the root bark of Flemingia philippinensis yielded eight inhibitory molecules (1-8) capable of targeting PTP1B. Three of them were identified to be novel compounds, philippin A (1), philippin B (2), and philippin C (3) which have a rare 3-phenyl-propanoyl chromenedione skeleton. The other compounds (4-8) were known prenylated isoflavones. All compounds (1-8) inhibited PTP1B in a dose dependent manner with IC(50)s ranging between 2.4 and 29.4 mu M. The most potent compound emerged to be prenylated isoflavone 5 (IC50 = 2.4 mu M). In kinetic studies, chromenedione derivatives (1-3) emerged to be reversible, competitive inhibitors, whereas prenylated isoflavones (5-8) were noncompetitive inhibitors. (C) 2015 Elsevier Ltd. All rights reserved.
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