Abstract: OBJECTIVE To review the pharmacological mechanism of hyperoside in anti-tumor and antioxidant, provide ideas for futher study of hyperoside finding out potential therapeutic targets and developing, so then to provide evidences for rational drug use in clinical. METHODS Through a large number of books and materials on hyperoside were reviewed to summarize its anti-tumor and antioxidant mechanisms etc. Summed up the hypericin anti-tumor mechanism and antioxidant effects. RESULTS Hypericin was an important natural product which widely distributed in the fruit of variety plants and the whole herbs. In recent years, it had been found that hyperoside could inhibit the growth of tumor cells, reduce the content of ROS in brain tissue and play an antioxidant role. In addition, hyperoside also had good performance in other aspects, such as antidepressant, heart/cerebral ischemia protection, liver preservation, immune regulation and so on. CONCLUSION Hyperin has a variety effects of anti-tumor, antioxidation etc, and its mechanism of action is clear. It has a broad development space.