Effects of transforming growth factor-beta (TGF-${eta}$) were investigated in human colorectal cancer, and the influence of cantharidinate in inhibiting TGF-${eta}1$ expression was explored. Relationships among TGF-${eta}1$ and sex, age, tumor size, tumor location, tumor stage were also analyzed. H&E and immunohistochemistry staining were employed to assess colorectal cancer and TGF-${eta}1$ expression, respectively. Then, HCT-116 CRC cells were randomly divided into four groups, controls, no serum-treated, chemotherapy and cantharidinate-treated. Immunohistochemistry and real-time PCR were employed to assess the expression of TGF-${eta}1$ in CRC cells. Our data showed that the expression of TGF-${eta}1$ might be associated with tumor size and tumor location (P<0.05). The expression of TGF-${eta}1$ in CRC groups was higher than in adjacent groups (P<0.05). In addition, the expression of TGF-${eta}1$ in cantharidinate-treated group was much lower than in CRC group (P<0.05). Taken together, these results suggest that TGF-${eta}1$ plays an important role in CRC development. Cantharidinate might inhibit the expression of TGF-${eta}1$ and control the development of colorectal cancer.