Gynura bicolor (Willd.) DC., is used in folk recipes for the treatment of diabetes mellitus in Jiangsu, Zhejiang and Sichuan province in the south of China. A previous pharmacological study proved that the plant showed significant hypoglycemic activity on normal and alloxan-diabetic mice. In this study, two terpenes, four megastigmane-type norisoprenoids and two glycosides were isolated from the aqueous ethanolic extract of the aerial parts of Gynura bicolor and characterized mainly by NMR spectroscopy and mass spectrometry. Thes e compounds were isolated for the first time from this plant, and no evidence could be found for the previous reported presence of megastigmane-type norisoprenoids in the genus Gynura.