AI Article Synopsis
- A study synthesized 29 phenylpropanoids to test their effectiveness as farnesoid X receptor (FXR) agonists in HepG2 cells using a dual-luciferase assay.
- Three compounds—auraptene, nelumol A, and nelumal A—demonstrated comparable potency to the natural ligand chenodeoxycholic acid (CDCA), with nelumal A showing slightly greater efficacy.
- Nelumal A is highlighted as a promising candidate for further research as a novel FXR agonist.
Article 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.
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| http://dx.doi.org/10.1016/j.bmcl.2012.03.057 | DOI Listing |
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