期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 9, 页码 3130-3135出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.03.057
关键词
Oxyprenylated natural phenylpropanoids; Farnesoid X receptors; Nelumal A; Ligularia nelumbifolia
资金
- University 'G. D'Annunzio' of Chieti-Pescara
A series of 29 oxyprenylated and azoprenylated phenylpropanoids were chemically synthesized and tested in transfected cultured HepG2 cells by means of the dual-luciferase assay as farnesoid X receptor (FXR) agonists, using the endogenous ligand chenodeoxycholic acid (CDCA) as reference drug. Among the tested molecules, three compounds, namely auraptene, nelumol A, and nelumal A showed a potency comparable to the endogenous ligand, with the latter natural product having a level of activity slightly superior to CDCA. Nelumal A is thus of interest as a valuable potential novel lead compound in the search for FXR agonists. (C) 2012 Elsevier Ltd. All rights reserved.
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