Diacerein: Recent insight into pharmacological activities and molecular pathways

Almezgagi, Maged; Zhang, Yu; Hezam, Kamal; Shamsan, Emad; Gamah, Mohammed; Al‐Shaebi, Fadhl; Abbas, Abdul Baset; Shoaib, Muhammad; Saif, Bassam; Han, Ying; Jia, Ru; Zhang, Wei

doi:10.1016/j.biopha.2020.110594

Cited by 60 publications

(34 citation statements)

References 77 publications

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“…Among them, Dahuang Lidan Jiaonang is used to treat acute cholecystitis [ 120 ] and nonalcoholic fatty liver [ 121 ], and Jiuzhi Dahuang Wan is applied to treat cirrhosis ascites [ 122 ]. Diacerein is a marketed drug for osteoarthritis, which has unique pharmacological actions and biological activities including anti-inflammatory, anticatabolic, and proanabolic properties on cartilage and synovial membrane clinically [ 123 ]. Furthermore, rhein is an active metabolite of diacerein [ 124 , 125 ] and the only analyte detected in human plasma at present [ 126 ].…”

Section: Conclusion and Discussionmentioning

confidence: 99%

Update on Pharmacological Activities, Security, and Pharmacokinetics of Rhein

Chen

Zhang

et al. 2021

Evidence-Based Complementary and Alternative Medicine

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Rhein, belonging to anthraquinone compounds, is one of the main active components of rhubarb and Polygonum multiflorum. Rhein has a variety of pharmacological effects, such as cardiocerebral protective effect, hepatoprotective effect, nephroprotective effect, anti-inflammation effect, antitumor effect, antidiabetic effect, and others. The mechanism is interrelated and complex, referring to NF-κB, PI3K/Akt/MAPK, p53, mitochondrial-mediated signaling pathway, oxidative stress signaling pathway, and so on. However, to some extent, its clinical application is limited by its poor water solubility and low bioavailability. Even more, rhein has potential liver and kidney toxicity. Therefore, in this paper, the pharmacological effects of rhein and its mechanism, pharmacokinetics, and safety studies were reviewed, in order to provide reference for the development and application of rhein.

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Section: Conclusion and Discussionmentioning

confidence: 99%

Update on Pharmacological Activities, Security, and Pharmacokinetics of Rhein

Chen

Zhang

et al. 2021

Evidence-Based Complementary and Alternative Medicine

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“…Therefore, one can assume that inflammation plays a vital role in myopia progression. Diacerein is an anti-inflammatory drug that is an inhibitor of proinflammatory IL-1β [24][25][26][27]. Diacerein may have therapeutic applications to attenuate cytokineinduced development of myopia progression.…”

Section: Discussionmentioning

confidence: 99%

Diacerein Inhibits Myopia Progression through Lowering Inflammation in Retinal Pigment Epithelial Cell

Tien

Lin

Chen

et al. 2021

Mediators of Inflammation

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Myopia is a highly prevalent refractive disorder. We investigated the effect of diacerein on monocular form deprivation (MFD) in hamsters as a possible therapeutic intervention. Diacerein is an anthraquinone derivative drug whose active metabolite is rhein. Diacerein or atropine was applied to the MFD hamsters, and their refractive error and axial length were measured after 21 days. The refractive error (control: − 0.91 ± 0.023 , atropine: − 0.3 ± 0.08 , and diacerein: − 0.27 ± 0.07 D ) and axial length (control: 0.401 ± 0.017 , atropine: 0.326 ± 0.017 , and diacerein: 0.334 ± 0.016 mm ) showed statistically significant differences between control, atropine-treated, and diacerein-treated MFD eyes. Furthermore, we determined the level of transforming growth factor-beta- (TGF-) β1, matrix metalloproteinase- (MMP-) 2, type I collagen, interleukin- (IL-) 6, IL-8, and monocyte chemoattractant protein- (MCP-) 1 in the retina. Atropine and diacerein suppressed levels of the myopia-related TGF-β1 and MMP-2 while increasing type I collagen expression. They also inhibited the interleukin IL-6, IL-8, and MCP-1 levels. Diacerein reduced the IL-6, IL-8, and MCP-1 expression in ARPE-19 cells. Furthermore, diacerein inhibited inflammation by attenuating the phosphorylation of protein kinase B (AKT) and nuclear factor kappa-light-chain-enhancer of activated B (NF-κB) pathway. This suggests that diacerein has a therapeutic effect on myopia and is a potential treatment option.

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“…As diacerein is well known for its antiosteoarthritis effects, numerous works analyzed its functions in preclinical and clinical settings. For a comprehensive review on such effects, the reader can refer to two recent works that analyzed extensively the antiosteoarthritis properties of diacerein [ 111 , 112 ]. Nonetheless, a very recent clinical trial compared diacerein to celecoxib in patients affected by knee osteoarthritis [ 113 ].…”

Section: Main Anthraquinones With Therapeutic Propertiesmentioning

confidence: 99%

An Update of Anthraquinone Derivatives Emodin, Diacerein, and Catenarin in Diabetes

Martorell

Castro

Victoriano

et al. 2021

Evidence-Based Complementary and Alternative Medicine

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Diabetes is part of metabolic diseases and is characterized by high blood sugar levels over a prolonged period as result of an insulin-deficient production or an inappropriate response to insulin by our cells. This chronic disease was the direct cause of 1.6 million deaths in 2016 as reported by the World Health Organization. Emodin is a natural product and active ingredient of various Chinese herbs with the chemical formula 1,3,8-trihydroxy-6-methylanthraquinone. Diacerein is another naturally occurring anthraquinone (1,8-diacetoxy-3-carboxyanthraquinone) commonly used as commercial drug to treat osteoarthritis. These two anthraquinone derivatives have been shown to exert antidiabetic activities. Emodin seems to enhance the glucose tolerance and insulin sensibility via activation of PPARγ and modulation of metabolic-related genes. Diacerein seems to decrease inflammatory cytokines and increase insulin secretion enhancing insulin sensibility and therefore improving glucose control. Other naturally occurring anthraquinone derivatives, such as catenarin (1,4,6,8-tetrahydroxy-3-methylanthraquinone), have been shown to have antidiabetic activities although few studies have been performed. The synthesis of new emodin derivatives is increasing, but these new molecules have not been tested for diabetes treatment. In the current work, available literature on anthraquinone derivatives' effects in diabetes disease is reviewed. Moreover, we discuss the chemistry, food sources, bioavailability, and toxicity of the naturally occurring anthraquinone with antidiabetic effects.

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Diacerein: Recent insight into pharmacological activities and molecular pathways

Cited by 60 publications

References 77 publications

Update on Pharmacological Activities, Security, and Pharmacokinetics of Rhein

Update on Pharmacological Activities, Security, and Pharmacokinetics of Rhein

Diacerein Inhibits Myopia Progression through Lowering Inflammation in Retinal Pigment Epithelial Cell

An Update of Anthraquinone Derivatives Emodin, Diacerein, and Catenarin in Diabetes

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