Micheliolide is a kind of guaiacane sesquiterpene lactone from natural plants. It distributs in the root bark of Cephalantheropsis gracilis and Michelia compressa . Modern pharmacological studies show that ，micheliolide can play an anti-tumor role by inhibiting the proliferation of tumor cells ，regulating the apoptosis of tumor cells ，inducing autophagy of tumor cells ，and inhibiting invasion and metastasis of tumor cells. It can reduce the expression of inflammatory cytokines by regulating several related signaling pathways ，such as nuclear factor κB and phosphatidylinositol-3-hydroxykinase/protein kinase B ；it can play an immunomodulatory role by restoring the expression of immune-related factors in the body ；it can play a neuroprotective effect by reducing the accumulation of amyloid β-protein and inhibiting microglial activation ；it can play a liver protective role by reducing the inflammatory response and steatosis of hepatocytes ；its nephroprotective mechanism is related to the relief of the inflammatory response by regulating multiple pathways ；the mechanisms of its cardioprotective action include alleviating the inflammatory response and reducing the level of oxidative stress ，etc. In conclusion ，micheliolide is a compound of great development value.