Micheliolide

Micheliolide is a sesquiterpene lactone and derivative of parthenolide (Item No. 70080) that has been found in M. champaca and has diverse biological activities.^1,2,3,4 It is an irreversible activator of the pyruvate kinase M2 isoform (PKM2; EC₅₀ = 6 nM) that decreases viability of HL-60 cells when used at concentrations ranging from 5 to 20 µM.¹ Micheliolide (5-10 µM) reduces M. tuberculosis-induced secretion of IL-1β and TNF-α, expression of Cox2, and production of nitric oxide (NO) in RAW 264.7 cells.² It also inhibits M. tuberculosis-induced NOD-, LRR-, and pyrin domain-containing protein 3 (NLRP3) inflammasome activation in RAW 264.7 cells. Micheliolide (30 mg/kg) decreases the severity of collagen-induced arthritis (CIA) in a mouse model of rheumatoid arthritis.³ It also increases hepatic protein levels of PPARγ and reduces hepatic inflammation and steatosis in db/db mice.⁴

WARNING This product is not for human or veterinary use.

1. Li, J., Li, S., Guo, J., et al. Natural product micheliolide (MCL) irreversibly activates pyruvate kinase M2 and suppresses leukemia. J. Med. Chem. 61(9), 4155-4164 (2018).

2. Zhang, Q., Jiang, X., He, W., et al. MCL plays an anti-inflammatory role in Mycobacterium tuberculosis-induced immune response by inhibiting NF-κB and NLRP3 inflammasome activation. Mediators Inflamm. 2432904 (2017).

3. Xu, H., Wang, J., Wang, C., et al. Therapeutic effects of micheliolide on a murine model of rheumatoid arthritis. Mol. Med. Rep. 11(1), 489-493 (2015).

4. Zhong, J., Gong, W., Chen, J., et al. Micheliolide alleviates hepatic steatosis in db/db mice by inhibiting inflammation and promoting autophagy via PPAR-γ-mediated NF-кB and AMPK/mTOR signaling. Int. Immunopharmacol. 59, 197-208 (2018).