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micheliolide
- Development stage
- Preclinical
- Lead developer
- University of Rochester
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Oral, Intraperitoneal, Intravenous, Rectal
01
Overview
Micheliolide is a natural sesquiterpene lactone isolated from plants such as Michelia compressa and Michelia champaca. It exhibits notable anti-cancer and anti-inflammatory activities. Mechanistically, micheliolide inhibits the NF-kappaB pathway and modulates other signaling pathways including PI3K/Akt and MAPK. It has demonstrated efficacy in preclinical models of cancer (notably acute myelogenous leukemia), inflammatory diseases like inflammatory bowel disease (IBD), rheumatoid arthritis models in mice, renal fibrosis models and colitis-associated cancer. Micheliolide selectively targets cancer stem cells and progenitor cells with cytotoxic effects while sparing normal hematopoietic stem cells. Its prodrug form dimethylaminomicheliolide (DMAMCL) is more stable in vivo and has advanced to clinical trials for glioblastoma[1][2][3][5][7][9].
- Other names
- (3aS,9R,9aS,9bS)-9-hydroxy-6,9-dimethyl-3-methylene-4,5,7,8,9a,9b-hexahydro-3aH-azuleno[4,5-b]furan-2-one68370-47-8
02
Targets
STAT3 (Signal Transducer and Activator of Transcription 3)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)PKM2 (Pyruvate kinase M2 isoform)STAT5A (STAT5)NF-κB
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