In recent years, the utilization of Chinese native medicine and other plant extracts in the treatment of diseases has attracted extensive attention, especially in the area of malignant tumors. However, lots of herbal remedies active ingredients have not been found or have been discovered but not effectively developed and applied. Therefore, screening new Chinese medicine active components and determining their antitumor effects have become a new breakthrough in the prevention and treatment of tumor disease. In the past years, a large number of studies have demonstrated that Polygonum cuspidatum and its active components like resveratrol showed excellent antitumor activities, including our own antitumor studies about resveratrol in colorectal cancer. The purpose of this review is to summarize the research progress of Chinese herb Polygonum cuspidatum and its active components in tumor diseases and provide theoretical basis for further scientific experiments and clinical applications.