Ethyl acetate-and n-butanol-soluble fractions of the leaves of Morus insignis showed a significant hypoglycemic activity on streptozotocin (STZ)-induced hyperglycemic rats. From these hypoglycemic activity-showing fractions, two new compounds, mulberrofuran U (2) and moracin M-3'-O-β-D-glucopyranoside (3) were isolated, along with six known compounds [β-sitosterol, β-sitosterol-3-O-β-glucopyranoside, ursolic acid, moracin M (1), kaempferol-3-O-β-glucopyranoside and quercetin-3-O-β-glucopyranoside] and the structures of the new compounds were determined by spectroscopic and chemical methods.