Recent advances in the studies on derivatives of five kinds of water-soluble pentacyclic tri-terpenoid acids has been reviewed.Pentacyclic triterpenoid acid possesses various biological activites.However,it is limited in the clinical application due to its poor solubility and low bioavailability.Therefore,it has become an interesting subject for the researchers to use pentacyclic triterpenoid acids as lead compounds to synthesize the water-soluble derivatives and to search for the candidate compounds having bioactivities and clinical value.