Alisma orientale (Sam.) Juzep. (Alismataceae) is a traditional and famous Chinese medicinal herb. Its rhizomes, which possess versatile bioactivities, are commonly used to treat oliguria, edema, gonorrhea with turbid urine, leukorrhea, diarrhea and dizziness. Approximately 120 compounds have been isolated from A. orientale. Terpenoids have been identified as A. orientale's characteristic constituents, which include protostane triterpenoids and guaiane sesquiterpenoids. The traditional medical uses of A. orientale in TCM have been evaluated in modern pharmacological studies, which have shown that A. orientale and its active constituents exhibit a wide range of bioactivities, such as diuretic, anti-urolithiatic, antinephritic, anti-atherosclerotic, immunomodulatory, and hepatoprotective activities. The medicinal potential of A. orientale makes it an ideal candidate for new drug development. Further studies are still required to identify its bioactive constituents, and elucidate the structure-activity relationship and detailed mechanisms of action. Additionally, the use of the other medicinal parts of A. orientale may reduce resource waste and afford novel secondary metabolites.