Inflammatory mediators and inflammatory cells in the inflammatory microenvironment promote the transformation of normal cells to cancer cells in the early stage of cancer, promote the growth and development of cancer cells, and induce tumor immune escape. The monomeric active ingredient β‐elemene is extracted from the traditional Chinese medicine Curcuma wenyujin and has been proven to have good anti‐inflammatory and antitumor activities in clinical applications for more than 20 years in China. Recent studies have found that this traditional Chinese medicine plays a vital role in macrophage infiltration and M2 polarization, as well as in regulating immune disorders, and it even regulates the transcription factors NF‐κB and STAT3 to alter inflammation, tumorigenesis, and development. In addition, β‐elemene regulates not only different inflammatory factors (such as TNF‐α, IFN, TGF‐β, and IL‐6/10) but also oxidative stress in vivo and in vitro. The excellent anti‐inflammatory and antitumor effects of β‐elemene and its ability to alter the inflammatory microenvironment of tumors have been gradually elaborated. Although the study of monomeric active ingredients in traditional Chinese medicines is insufficient in terms of quality and quantity, the pharmacological effects of more active ingredients of traditional Chinese medicines will be revealed after β‐elemene.