Anthraquinones, especially hydroxyanthraquinones, constitute one of the most ubiquitous classes of naturally occurring phenolic compounds. The hydroxyl and aminoanthraquiones show diverse physiological and pharmacological activity. Since pharmacological studies of small molecule bioactive compounds are known to be hampered by their weak solubility in water, it is important to prepare water-soluble analogues of hydroxy- and aminoanthraquinones by biotransformation. This review summarizes the glucosidation of substituted anthraquinones to achieve soluble analogues using fungi.