Abstract: Amino acids, as the basic constituent units of biological macromolecular proteins, participate in the processes of metabolic regulation and information transmission in the body.In recent years, studies have found that the use of amino acids to modify active ingredients of traditional Chinese medicine with antitumor effects, such as arctigenin, oleanolic acid, podophyllotoxin, betulin, and betulinic acid, can improve the solubility of active ingredients of traditional Chinese medicine, increase bioavailability, and improve the targeting of tumor cells.This article summarizes the research progress and application of amino acid modification of active ingredients in Chinese medicine with antitumor effects.