Abstract: Immune cells are involved in regulating the pathogenesis and development of major human diseases such as autoimmune diseases, tumors and infections. A large number of studies have shown that many natural products derived from traditional Chinese medicine have regulatory effects on immune cells, suggesting that they may become potential drugs for the treatment of diseases related to the immune system. This article reviewed the latest research progress in the immunoregulatory roles of natural products and summarized natural small-molecule drugs targeting immune cells, so as to promote related drug development and provide new ideas for the treatment of immune-related diseases.