The invention discloses glycosyl beta-elemene derivatives having general formulae I, II and III. Researches indicate that the glycosyl beta-elemene derivatives have good biological water solubility and good anti-cancer activities, can be applied to malignant tumor treatment as an anti-cancer medicine for realizing real-time tumor monitoring and treatment, and have important scientific meaning to researches and application of beta-elemene in the field of medicine. Furthermore, the invention provides a method for preparing the corresponding compounds. The method applies a click chemical reaction technology, and is simple and scientific in synthesis.