Abstract: Chronic inflammation is closely related to the occurrence, development, invasion and metastasis of tumors. Hedyotis diffusa Willd. has both anti-inflammatory and anti-tumor effects and is often used to prevent and treat various kinds of inflammation and tumors. The anti-inflammatory mechanism of Hedyotis diffusa Willd. is related to NF-κB, MAPK, 5-LOX and other signaling pathways and the anti-tumor effects include anti-colon cancer, anti-lung cancer, anti-liver cancer, anti-breast cancer, anti-gastric cancer, etc and anti-tumor mechanisms include signaling pathways such as PI3K/AKT, TGF-/Smad, MAPK, STAT3. Hedyotis diffusa Willd. plays an important role in the process of "inflammation-cancer" transformation through NF-κB, MAPK, VEGF and so on. This study provides a reference for the further research and development of the anti-inflammatory, anti-tumor properties and intervention on "inflammation-cancer" transformation of Hedyotis diffusa Willd.