Aminoside tetracyclic anthraquinones represented by formula (I) and (II). Peptides are introduced to connect tetracyclic anthraquinones and fatty acid to enable selective absorption and release of the anticancer agents. In addition, aminosaccharide and tetracyclic moieties are introduced into the branched chain to improve water-solubility. The compounds of formula (I) and (II) are pharmaceutically active components useful for treating diseases that are cured by aminoside tetracyclic anthraquinones, including cancer.
