The present invention provides aminoside tetracyclic anthraquinones represented byformula I or II, wherein the piptides are introduced to connect tetracyclic anthraquinonesand fatty acid saturated or unsaturated in order to make the anticancer agentsto be absorbed and released selectively; meanwhile some water-solubility groupsare also introduced into the branched chain, aminosaccharide and tetracyclic moietyof the compounds to improve the water-solubility. The present invention alsoprovides the preparative method and the use thereof as pharmaceutically activecomponents for treating the diseases cured by aminoside tetracyclic anthraquinone,for example cancer, such as intestines, liver, gastric, breast, lung, ovary,prostate, brain glioma, lymph, skin, pigment, thyroid gland, multiple bonemarrow cancer and leukemia.