Abstract: Oxidative stress related diseases affect people’s health. Nrf2-Keap1-ARE signaling pathway plays a vital role in the regulation of cellular oxidative stress response, and the downstream phase II detoxification enzymes, antioxidant enzymes and transporters are involved in tumor resistance and anti-oxidative stress. This paper focuses on the structure and function of Nrf2 and Keap1, the regulating mechanism of Nrf2-Keap1-ARE signaling pathway, and introduces effective components of Chinese medicine which can act on the Nrf2-Keap1-ARE signaling pathway. We aim to provide a theoretical basis for the clinical use of traditional Chinese medicine and its effective components, which can be used on prevention and treatment of oxidative stress related diseases.