Micheliolide has antineoplastic, anti-inflammatory and immunomodulatory effects, it inhibits various inflammatory response and may serve as a neuroprotective agent in neuroinflammation-related neurodegenerative disorders. Micheliolide has potential as a candidate drug for the treatment of diabetic nephropathy, it can effectively attenuate the high glucose-stimulated activation of NF-κB, the degradation of IκBα, and the expression of MCP-1, TGF-β1 and FN in rat mesangial cells (MCs). Micheliolide also ameliorates liver steatosis by upregulating PPAR-γ expression, thereby inhibiting NF-κB-mediated inflammation and activating AMPK/mTOR-dependent autophagy.