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Amorfrutins are potent PPARγ modulators. (A) Structures of four amorfrutins described in this study and lead structure. R1: Isoprenoyl residues; R2: H or Me; R3: H or isoprenoyl residues; R4: H, aliphatic or aromatic residues or a combination thereof. (B) Binding of compounds on PPARγ-LBD in a competitive TR-FRET assay. (C) Cellular activation of PPARγ determined in a reporter gene assay in HEK 293H cells.
