title: Nelumal A, the active principle from Ligularia nelumbifolia, is a novel farnesoid X receptor agonist.
abstract: 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.
authors.affiliation: Dipartimento di Scienze del Farmaco, Università G. D'Annunzio Chieti-Pescara, Via dei Vestini 31, 66100 Chieti Scalo (CH), Italy. fepifano@unich.it
authors.forename: Francesco
authors.initials: F
authors.lastname: Epifano
authors.forename: Salvatore
authors.initials: S
authors.lastname: Genovese
authors.forename: E
authors.initials: E
authors.lastname: James Squires
authors.forename: Matthew A
authors.initials: MA
authors.lastname: Gray
mesh_terms: D000475:Alkenes; D019659:Asteraceae / Q000737:chemistry*; D045744:Cell Line, Tumor; D055088:Early Detection of Cancer; D006801:Humans; D010936:Plant Extracts / Q000737:chemistry* / Q000494:pharmacology; D054876:Prenylation; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists*; D000099150:Receptor, Farnesoid X-Activated
chemical_list: D000475:Alkenes; D010936:Plant Extracts; D018160:Receptors, Cytoplasmic and Nuclear; D000099150:Receptor, Farnesoid X-Activated; C013658:propylene