Description
Diacerein is an anthraquinone that exhibits antinociceptive, anti-inflammatory, and anti-resorptive activities. Diacerein is clinically used to treat osteoarthritis. In vivo, diacerein inhibits IL-1β as well as somatic nociception induced by glutamate, NMDA, and kainate. In vitro, diacerein decreases expression of matrix metalloproteinase 13 (MMP13), cathepsin K, ERK1/2, and p38 MAPK, resulting in decreases in the synthesis of resorptive factors and in osteoclast formation. In other cellular models, diacerein inhibits IL-1.
References
Gadotti VM, Martins DF, Pinto HF, et al. Diacerein decreases visceral pain through inhibition of glutamatergic neurotransmission and cytokine signaling in mice. Pharmacol Biochem Behav. 2012 Oct;102(4):549-54. PMID: 22750064.
Boileau C, Tat SK, Pelletier JP, et al. Diacerein inhibits the synthesis of resorptive enzymes and reduces osteoclastic differentiation/survival in osteoarthritic subchondral bone: a possible mechanism for a protective effect against subchondral bone remodelling. Arthritis Res Ther. 2008;10(3):R71. PMID: 18578867.
Fidelix TS, Soares BG, Trevisani VF. Diacerein for osteoarthritis. Cochrane Database Syst Rev. 2006 Jan 25;(1):CD005117. PMID: 16437519.
