Diacerein, an anti-OA agent, can significantly inhibit IL-1β production. Both nitric oxide (NO) release and IL-1βsecretion induced by LPS could be reduced by treatment with 1μM Diacerein in human OA synovial tissue. Similar effect of Diacerein could be observed in LPS stimulated human cartilage in culture[1]. The synthesis of MMP-13 induced by IL-1β could be dose-dependently reduced by Diacerein at concentration of 10 and 20μg/ml in subchondral bone explants. Pre-incubation with diacerein for 2 hours with diacerein at 20 μg/mL led to inhibition of ERK1/2 and p38 pathways activated by IL-1β at concentration of 100 pg/mL for 30 minutes in the OA subchondral bone osteoblasts. Differentiation/proliferation of osteoclasts Raw 264.7 cells under RANKL treatment and IL-1β stimulation could be markedly inhibited by 20 μg/mL Diacerein[2].
Diacerein/双醋瑞因 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Chondrocytes
10 μmol/L
24 hours
To evaluate the effect of Diacerein on IL-1β-induced chondrocyte apoptosis. Results showed that Diacerein and its nanoformulations significantly reduced chondrocyte apoptosis and exerted protective effects by regulating Bcl-2, Bax, and caspase-3 protein expression.
Acta Pharm Sin B. 2024 Nov;14(11):5008-5025.
Mouse primary hepatocytes
40 μM
30 min pretreatment, followed by LPS stimulation for 4 h and cholesterol stimulation for 12 h
Diacerein inhibited IL-1β secretion and LDH release but had no effect on TNF-α; inhibited caspase-1 cleavage
J Transl Med. 2022 Jun 28;20(1):294.
Mouse Kuffer cells
40 μM
30 min pretreatment, followed by LPS stimulation for 4 h and cholesterol stimulation for 12 h
Diacerein inhibited IL-1β secretion but had no effect on TNF-α; inhibited ASC speck formation
J Transl Med. 2022 Jun 28;20(1):294.
Mouse bone marrow-derived macrophages (BMDMs)
40 μM
30 min pretreatment, followed by LPS stimulation for 4 h and nigericin stimulation for 2 h
Diacerein inhibited IL-1β secretion but had no effect on TNF-α; inhibited caspase-1 cleavage and ASC speck formation
J Transl Med. 2022 Jun 28;20(1):294.
Diacerein/双醋瑞因 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
Destabilized medial meniscus (DMM)-induced osteoarthritis model
Intra-articular injection
2 mg/kg
Once weekly for 3 weeks
To evaluate the therapeutic effect of Diacerein nanoformulations on osteoarthritis. Results showed that Diacerein nanoformulations significantly improved joint degeneration, reduced cartilage damage, and alleviated pain.
Acta Pharm Sin B. 2024 Nov;14(11):5008-5025.
C57BL/6 mice
NAFLD model induced by methionine and choline deficiency diet (MCD)
Gavage
15 mg
Every 2 days for 3 weeks or 9 weeks
Diacerein improved liver function (ALT and AST), serum inflammation (IL-1β and TNF-α), histopathological inflammation score, and liver fibrosis
J Transl Med. 2022 Jun 28;20(1):294.
BALB/c mice
Acetaminophen-induced hepatotoxicity model
Intraperitoneal injection
20 mg/kg
Single administration, total experimental period was 36 hours
To evaluate the preventive and curative effects of Diacerein on acetaminophen-induced hepatotoxicity. Results showed that Diacerein significantly reduced biomarkers of liver dysfunction, oxidative stress, hepatocyte necrosis, and infiltration of neutrophils and macrophages whether administered 4 h before or 2 h after acetaminophen. Further, Diacerein counteracted acetaminophen-induced hepatocellular apoptosis by increasing Bcl-2 and decreasing Bax and caspase-3 expression levels. Moreover, DCN normalized hepatic TNF-α and significantly decreased NF-κB p65 expression.
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