Biological Characteristics of Micheliolide and Its Neuroprotective / Anti-inflammatory Activity
1. Department of Immunology and Microbiology, School of Integrative Medicine, Shanghai University of TCM, Shanghai 201203, China
2. Shanghai Key Laboratory of Health Identification and Assessment, Shanghai University of TCM, Shanghai 201203, China
| Abstract: | Sesquiterpene lactones (SLs) isolated from natural medicinal plants have been traditionally used to treat numerous dis-eases, especially chronic inflammatory diseases in folk medicine. Dietary vegetables, such as lettuce and chicory are also important sources of SLs in daily life. Micheliolide (MCL) is a recently discovered SL from Compositae plants. MCL can also be semi-synthesized from parthenolide, and undergo a biological, chemical transformation to dimethylamino micheliolide (DMAMCL) and ACT001 for higher bioavailability and better biological function. Systematic pharmaco-kinetic researches showed that MCL and its derivatives were widely distributed in the heart, spleen, lung, kidney, brain, stomach, duodenum, testicle, fat, marrow, and muscle within 30 min, concentration reaches peak approximately at 1 h and significantly reduces 3 h later in a majority of tissues. MCL has been shown to have a good therapeutic effect on various cancers, diabetic nephropathy, nervous system disease, bacterial infectious disease, and autoimmune disease through immune response regulation, such as inhibition of NF-кB, PI3K/AKT/mTOR and MAPK signaling pathways. MCL also showed a good blood-brain barrier permeability, and have the neuroprotective effect on stroke and Alzhei-mer's disease. Yet, the exact molecular mechanism of MCL remains unclear. Identification of relevant targets (such as pyruvate kinase muscle type 2 (PKM2)) also represents a great challenge for researchers. The biological characteristics, major biological activities, and molecular mechanisms of MCL were summarized in this review, indicating the potential clinical application for inflammatory and infectious diseases. |
| Keywords: | Micheliolide; Sesquiterpene Lactones; Anti-cancer; Anti-inflammation; Immunoregulation |
| DOI: | 10.57237/j.jsts.2025.02.001 |
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Received: 13 April 2025
Accepted: 10 July 2025
Published Online: 1 August 2025
Funding
| 1. | Shanghai Key Laboratory of Health Identification and Assessment (21DZ2271000) |
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