OBJECTIVE: To evaluate the effects of luteolin on the expressions of TGF-β1R II, NF-κB, and VEGF genes in tumor tissues of mice with H29 colon cancer. STUDY DESIGN: Fifty ICR mice with H29 colon cancer were randomly divided into 5 groups: normal saline group, low-dose luteolin group, middle-dose luteolin group, high-dose luteolin group, and cyclophosphamide group. The mice were killed on the day after administration discontinuance, and subcutaneous tumor tissues were collected. Quantitative fluorescence RT-PCR was used to detect the expressions of TGF-β1R II, NF-κB, and VEGF genes. RESULTS: Luteolin raised the expression level of TGF- β1R II in H29 colon cancer tissues, which showed the most obvious effect in the middle-dose group compared with that of the normal saline group (p < 0.01). The luteolin group of each dose significantly lowered the NF-κB expression level in H29 colon solid tumors, showing significant differences compared with that of the normal saline group (p < 0.01). The middle-dose and high-dose luteolin groups significantly reduced the level of VEGF expression, and the high-dose group had the most obvious effect. There were significant differences among the middle-dose group, high-dose group, and normal saline group (p < 0.01). CONCLUSION: Luteolin may exert antitumor effects by elevating the expression of TGF-β1R II through downregulating those of NF-κB and VEGF in tumor tissues of mice with H29 colon cancer, thereby inhibiting tumor angiogenesis and tumor cell proliferation. © Science Printers and Publishers, Inc.