Sappanchalcone is a flavonoid isolated from Caesalpinia sappan L, a potent low-toxicity Fibroblast activation protein α (FAPα) inhibitor with SPR KD of 3.88 uM.
Sappanchalcone not only inhibits FAPα enzymatic activity but also effectively downregulates its protein expression under fibrotic conditions.
Sappanchalcone displays inhibition of LX -2 cell proliferation, effectively inhibits the migration and invasion of activated hepatic stellate cells (aHSCs), demonstrating excellent anti -fibrotic potential.
Sappanchalcone suppresses hepatic stellate cell activation through inhibition of the FAPα-PI3K-AKT signaling pathway.
Sappanchalcone markedly attenuates fibrosis progression and improves liver function in multiple liver fibrosis models using male mice.
Sappanchalcone demonstrates significant upregulation of α -SMA and FAPα proteins in the BDL model, both of which are effectively downregulated by Sappanchalcone.