Multidrug resistance (MDR) is the main factor of tumor recurrence and chemothera-py failure in clinical practice. Its mechanism is rela-tively complex, and one of the most thoroughly studied mechanism is the overexpression of P-gly-coprotein (P-gp) on tumor cell membrane. Most of the chemotherapy drugs are p-gp substrates, and tumor cells will transport the chemotherapy drugs to the extracellular through p-gp mediated active transport, so that the concentration of effective drugs in the cell is reduced, resulting in drug resis-tance, leading to the decline of clinical efficacy. The reversal agent of P-gp can reduce the intracellular pumping of chemotherapeutic drugs by regulating the expression and transport activity of P-gp, and enhance the sensitivity of tumor cells to chemo-therapeutic drugs, thus improving the therapeutic effect. In this paper, we will summarize the natural plant active ingredients that can reverse P-gp medi-ated MDR to provide reference for clinical and re-lated studies.