Dipartimento di Scienze del Farmaco, Università G. D'Annunzio Chieti-Pescara, Via dei Vestini 31, 66100 Chieti Scalo (CH), Italy.
Bioorg Med Chem Lett. 2012 May 1;22(9):3130-5. doi: 10.1016/j.bmcl.2012.03.057. Epub 2012 Mar 22.
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.
一系列 29 个氧代丙酰基和氮代丙酰基苯丙烷类化合物被化学合成，并通过双荧光素酶检测在转染的 HepG2 细胞中进行了测试，作为法尼醇 X 受体 (FXR) 的激动剂，以内源性配体鹅去氧胆酸 (CDCA) 作为参考药物。在所测试的分子中，三种化合物，即 Auraptene、Nelumol A 和 Nelumal A，表现出与内源性配体相当的效力，后一种天然产物的活性略高于 CDCA。因此，Nelumal A 作为寻找 FXR 激动剂的有价值的潜在新型先导化合物引起了人们的兴趣。
