Panax ginseng C.A.Meyer is one of traditional Chinese medicines. Ginsenosides are the main components of Panax ginseng with various benefit pharmacological actions. In the paper the advance of research on antitumour activity of ginsenosides, especially ginsenoside-Rg 3 and ginsenoside-Rh 2, were reviewed. The structure-activity relationship of ginsenosides on antitumour activity was discussed.The preparation of ginsenoside-Rg 3 and ginsenoside-Rh 2 with high activity of antitumour from other ginsenosides by glucogen reformation were discussed deeply. The trends of development of ginsenosides were put forward.