Background Cancer is one of the most serious diseases worldwide that threatens human health and leads to death. Chemotherapy is the main clinical method to treat tumors, but, despite the development of new chemotherapeutic drugs, the multidrug resistance (MDR) of cancer cells to conventional chemotherapeutic drugs remains a major cause of failure in cancer prevention and treatment. Therefore, overcoming this resistance has become a major challenge in cancer prevention and treatment. Method With the in-depth study of traditional Chinese medicines (TCMs) for the treatment of tumors, many such medicines have been found that can reverse MDR and enhance the sensitivity of chemotherapy. ZJW is a famous traditional medicine formula from China, recorded first in an ancient medicine book named Danxi Xinfa. It is composed of Huanglian and Wuzhuyu in a ratio of 6:1 by mass. Conclusion ZJW can inhibit proliferation, induce apoptosis, inhibit invasion and metastasis, and reverse MDR of tumor cells through multiple pathways and multiple targets. In this paper, we briefly review recent research on ZJW and its main components, evodiamine and berberine, in the anti-tumor mechanism and reversal of multidrug resistance.