Nelumal A, the active principle from Ligularia nelumbifolia, is a novel farnesoid X receptor agonist

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.