ArticleApplied biochemistry and biotechnology2026
Diacerein Protects Against Obesity-Related Cardiovascular Injury: Evidence from In Silico and In Vivo Studies.
Article in Applied biochemistry and biotechnology, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Obesity constitutes a significant worldwide health challenge and a primary risk factor for cardiovascular diseases. Diacerein, an anti-inflammatory medication approved for osteoarthritis, is being studied as a potential modulator of inflammatory signaling. However, its role in obesity-associated cardiovascular injury remains incompletely understood. In the present study, computational docking and 300-ns MD simulations supported preferential, stable binding of diacerein to the TLR4 complex through a deep, hydrophobic, solvent-shielded pose, consistent with coordinated protein dynamics. Then, the cardioprotective effects of diacerein were examined in a high-fat diet (HFD)-induced obesity model. Male Sprague-Dawley rats were divided into three groups: normal control, HFD, and HFD combined with diacerein (50 mg/kg/day) for 10 weeks. Metabolic parameters, lipid profile, serum troponin I, and C-reactive protein (CRP) were evaluated. A histopathological examination of the heart and aorta was conducted, and the tissue levels of TLR4, MyD88, IRAK1, TRAF6, NF-κB, and downstream pro-inflammatory cytokines (IL-6 and TNF-α) were assessed. Inflammatory cell infiltration was evaluated using CD45 immunohistochemistry. The HFD led to insulin resistance, dyslipidemia, increased troponin I and CRP levels, and significant histological alterations in cardiac and aortic tissues, accompanied by the activation of the TLR4/NF-κB inflammatory pathway and enhanced inflammatory cell infiltration. Diacerein treatment markedly alleviated metabolic abnormalities, diminished cardiac injury and systemic inflammation, improved histological features, and reduced tissue protein levels of the TLR4/NF-κB pathway and pro-inflammatory cytokines. In conclusion, diacerein provides marked protection against obesity-induced cardiovascular injury, at least partially, by inhibiting the TLR4/NF-κB inflammatory pathway, supporting its potential as a therapeutic strategy for obesity-related cardiovascular complications.
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