Abstract: Anthocyanidins, a type of water-soluble flavonoid pigment, are commonly present in fruits and vegetables. It has been demonstrated that anthocyanidins have various biological activities such as anti-inflammatory, antioxidant, antibacterial, etc. The stability and biological activity of anthocyanidins can be effectively improved by acylation, copigmentation, encapsulation, and other processes. Administering the drug directly for the treatment of oral diseases has a potential application that can successfully prevent drug bioavailability compromised by gastrointestinal digestion. This study reviewed the bioactivity features of anthocyanidins, bioactivity enhancement strategies, and their applications in the treatment of oral diseases, which could provide ideas and guidelines for further developing anthocyanidin-based medications to treat oral diseases.