Abstract: Gut is not only responsible for the digestion and absorption of foods, but also participates in the maintenance of homeostasis, the occurrence and progression of diseases, as well as the transportation and action of drugs through microbial, neuroendocrinal and immunologic communications with extra-gut tissues. Recently, it has been found that gut is the primary action site of several active constituents isolated from traditional Chinese medicine (TCM). For example, berberine, curcumin and resveratrol have been shown to exert their pharmacological effects through intestinal routes. This paper reviewed the research advances in intestinal routes involved in the action of TCM from the perspectives of gut microbiota, neuroendocrine and mucosal immunity.