Isofraxetin-6-O-β-d-glucopyranoside was deglycosylated using Angelica sinensis (Oliv.) Diels callus. A new coumarin was produced by the system with the stimulation of isofraxetin-6-O-β-d-glucopyranoside. Anti-inflammatory effects of transformed products were evaluated, and possible biosynthetic pathways were described.