Autophagy is an energy metabolism and self-update mechanism for maintaining the intracellular homeostasis. It is involved in many physiological and pathological processes in cells. The recent studies showed that autophagy is closely related to tumorigenesis and development. It participates in the regulation of tumor formation, proliferation, metastasis and energy metabolism. Autophagy's regulatory effect on tumors is a complex dynamic process. Autophagy can impede early cancer development, while promoting advanced tumor progress. In recent years, autophagy has become a new hotspot in the field of cancer research. At present, more and more studies showed that Chinese herbal medicines and their effective components could regulate autophagy in cancer cells. In response to the complex role of autophagy in cancer development, traditional Chinese medicines and their derived anti-cancer compounds also have multiple effects in autophagy regulation. Some of them can cause autophagic cell death, while others may inhibit autophagy metastasis or enhance tumor sensitivity to anti-cancer drugs by restraining autophagy process. They may show distinct effects in autophagic death or protective autophagy in different types of tumor. At present, studies on anticancer compounds with regulatory effect on tumor autophagy mainly focus on saponins, alkaloids, polyphenols, flavone and lactone. Their antitumor effects can be achieved by inducing autophagic death or autophagy suppression. In this paper, the effect and mechanisms of anti-cancer herbal medicines in regulating tumor cell autophagy were reviewed to help develop antitumor herbal drugs targeting autophagy and provide a new direction for anticancer drug development.