Two Types of PPARγ Ligands Identified in the Extract of Artemisia campestris

The 70% ethanol extract of Artemisia campestris was screened to find PPARγ ligands using the ligand-responsive chimera luciferase reporter system. Capillartemisin B identified as a ligand that stimulated lipid accumulation in 3T3-L1 cells. By further purification from large-scale preparation methanol campestris, we isolated and eupatilin santaflavone ligands. Weak activity or assay enhanced by antagonist, GW9662, suggesting GW9662 bound simultaneously multiple sub-pockets ligand-binding domain (LBD) cooperatively activated PPARγ. Docking simulation suggested binds Ω-pocket but not AF-2 pocket Y-shaped LBD where artepillin C differs capillartemisin at C-5′ position without hydroxy group binds. Eupatilin with did stimulate differentiated cells, binding each compound alone which PPARγ-responsive expression enough accumulation. found this study have potential design fragment-based drug novel cover LBD.