Diacerein

Diacerein (Diacerhein), an orally active anthraquinone, reduces production of IL-1 converting enzyme then inhibits the activation of IL-1β by related downstream signaling. Diacerein is an anti-inflammatory and anti-rheumatic drug. Diacerein can relieve bronchospasm and control airway inflammation in asthmatic mice. Diacerein has the potential for slow acting drug in osteoarthritis (SYSADOA) research^[1][2][3]. In Vitro: Diacerein (Diacerhein; 30-300 μM; 24, 48 h) reduces cell proliferation and viability of chondrosarcoma cells^[1].
Diacerine (30-300 μM; 48 h) causes a SW-1353 cell cycle G2/M arrest^[1].
Diacerein (30-300 μM; 48 h) decreases cyclin B1, CDK1, and CDK2 levels in SW-1353 cell^[1].
Diacerein can relax the agonist-precontracted mouse airway smooth muscle via intracellular and extracellular calcium mobilization which is mediated by switched voltage-dependent L-type Ca²⁺ channels, non-selective cation channels, large-conductance Ca²⁺-activated K⁺ channel, and Na⁺/Ca²⁺ exchangers^[2].
In Vivo: Diacerein (Diacerhein; 50, 100, 200 mg/kg; Gavaged; daily; a week) can effectively reduce airway hypertension and improve airway remodeling in asthmatic mice with Ovalbumin (OVA; 3 mg/ml; 200 μl; IP; dissolved with 25 mg/ml Al(OH)3 at day 1, day 8)^[2].
Diacerein (2, 20, 60 mg/kg; daily; oral; at 2 weeks of age transgenic mice; for 5 weeks) reveales a significant reduction not only in cartilage destruction but also in the extent of synovitis and bone erosion in the Tg197 transgenic murine model of RA^[3].