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Micheliolide (MCL) is a chief constituent of plants such as Magnolia grandiflora L. , Michelia compressa (Maxim.) Sarg . and Michelia champaca L. It is known to exhibit significant anticancer activity by various scientific investigations. This review aims to emphasize the anticancer and antiinflammatory activities of MCL. In this review, we summarized the published data in peer-reviewed manuscripts published in English. Our search was based on the following scientific search engines and databases: Scopus, Google Scholar, ScienceDirect, Springer, PubMed, and SciFinder, MCL possesses a broad spectrum of medicinal properties like other sesquiterpene lactones. The anticancer activity of this compound may be attributed to the modulation of several signaling cascades (PI3K/Akt and NF-κB pathways). It also induces apoptosis by arresting the cell cycle at the G1/G0 phase, S phase, and G2/M phase in many cancer cell lines. Very little data is available on its modulatory action on other signaling cascades like MAPK, STAT3, Wnt, TGFβ, Notch, EGFR, etc. This compound can be potentiated as a novel anticancer drug after thorough investigations in vitro , in vivo , and in silico -based studies., Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (© 2024 The Authors.)