Both in vitro and in vitro studies have proved that partial of Chinese materia medica including monomer or active ingredients have synergistic action with chemotherapeutic agents, the former could enhance the effect of the latter. Its mechanism may be correlated with the actions of Chinese materia medica in enhancing immune function, directly killing tumor cells, inducing tumor cell apoptosis, regulating cell cycle and reversing chemotherapeutic drug resistance, etc. The present article summarized the synergistic effect of Chinese materia medica, monomer or active ingredients, with various chemotherapeutic agents, and tried to provide a theoretical evidence for combined application of them in the procedure of clinical tumor treatment.