For research use only.
CAS No. 13739-02-1
Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis.
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|Description||Diacerein is an inhibitor of pro-inflammatory cytokine Interleukin-1B (IL-1B) production, prescribed for osteoarthritis and chronic inflammatory arthritis.|
Diacerein significantly inhibits LPS-induced IL-1beta production by synovial tissue and cartilage. Diacerein (1 μM) has a significantly less inhibitory effect on cartilage synthesis than culture media containing LPS only. Diacerein (1 μM) decreases NO release in synovial tissue and cartilage media and increases IL-1ra levels in cartilage culture media.  Diacerein (10 μM) enhances the expression of TGF-beta1 and TGF-beta2 in cultured bovine articular chondrocytes.  Diacerein reduces, in a dose-dependent manner, the interleukin-1-beta (IL-1beta)-induced MMP-13 production in osteoarthritic subchondral bone. Diacerein significantly reduces the activity of MMP-13 and cathepsin K in osteoclasts. Diacerein effectively blocks the IL-1beta effect on the osteoclast differentiation process and the survival of mature osteoclasts. 
|In vivo||Diacerein (100 mg/kg/day) significantly suppresses the paw edema and the increase in serum mucoprotein in the adjuvant-induced arthritic rats. Diacerein (30 mg/kg/day) combined with Naproxen (3 mg/kg/day) results in significantly greater anti-inflammatory activity than with naproxen alone in the adjuvant-induced arthritic rats. Diacerein (100 mg/kg/day) also significantly prevents bone loss and reduces the serum alkaline phosphatase and decreases the excretion of urinary hydroxyproline in the ovariectomized rats.  Diacerein (25 mg/kg) decreases the thickness of cartilage and subchondral bone in the lesion (middle) zone of the lateral tibial plateau in Merino wethers. |
-  Yaron M, et al. Osteoarthritis Cartilage, 1999, 7(3), 272-280.
-  Felisaz N, et al. Osteoarthritis Cartilage, 1999, 7(3), 255-264.
-  Boileau C, et al. Arthritis Res Ther, 2008, 10(3), R71.
|In vitro||DMSO||48 mg/mL (130.33 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03472287||Completed||Drug: Diacerein 1% Ointment||Epidermolysis Bullosa (EB)|Epidermolysis Bullosa Simplex|Dystrophic Epidermolysis Bullosa|Junctional Epidermolysis Bullosa||Castle Creek Pharmaceuticals LLC||May 18 2018||Phase 1|
|NCT03389308||Completed||Drug: diacerein 1% ointment||Epidermolysis Bullosa|Epidermolysis Bullosa Simplex||Castle Creek Pharmaceuticals LLC||December 1 2017||Phase 2|
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