To search for the anti-diabetic principle from the stem bark of Kalopanax pictus, seven kinds of chemical constituents including hederagenin glycosides and phenolic glycosides wre isolated. The anti-diabetic evaluation of these isoltes in the streptozotocin-induced diabetic rats exhibited that kalopanaxsaponin A has a potent anti-diabetic activity in contrast to a mild activity of hederagenin. In addition, significant hypocholesterolemic and hypolipidemic activities of kalopanaxsaponin A and hederagenin were observed. The structure-activity relationship of kalopanaxsaponin A was also investigated in the present work.