Abstract: With the rising of the morbidity and mortality rates, malignant tumor has become a major threat to human health. Due to the small chemical drugs made more difficulties in development, active peptides with many advantages, such as high efficiency and low toxicity, have received more attention. The characteristics, sources, preparation methods, structure modification and mechanism of peptide were summarized in this paper. The reference will be provided and helpful for future research work, especially to the current research of the peptides in clinical trials.