| Description | Diacerein (Fisiodar) is a prodrug which is metabolized to rhein. It is currently approved in France for the treatment of osteoarthritis although the use of diacerein is restricted due to the side effects including sevre diarrhea [L780]. Diacerein is under investigation for the treatment of Insulin Resistance, Diabetes Mellitus (Type 2), and Diabetes-Related Complications. |
| In vitro | 在卵巢切除大鼠中,每天100 mg/kg Diacerein明显防止骨损失并降低血清碱性磷酸酶,减少尿中羟脯氨酸的排泄. 每天100 mg/kg Diacerein明显抑制佐剂诱导的关节炎大鼠的爪水肿和血清粘蛋白的增加.在佐剂诱导的关节炎大鼠中,每天30 mg/kg Diacerein和每天3 mg/kg Naproxen联用比单独使用Naproxen表现更明显的抗炎活性.在Merino羊胫骨外侧平台的病变部位,25 mg/kg Diacerein减小软骨和软骨内骨的厚度. |
| In vivo | Diacerein明显降低破骨细胞中MMP-13和组织蛋白酶K的活性。Diacerein有效地阻断IL-1β对破骨细胞分化过程和成熟破骨细胞存活的影响。Diacerein明显抑制滑膜组织和软骨中脂多糖诱导的IL-1β生成。Diacerein以剂量依赖性方式减少骨关节炎软骨内骨中白细胞介素-1-β（IL-1β）诱导的MMP-13的生成。1 μM Diacerein对软骨合成的抑制作用明显低于仅含有LPS的培养基。1 μM Diacerein减少滑膜组织和软骨培养液中NO释放,增加软骨培养基的IL-1ra水平。10 μM Diacerein提高培养的牛关节软骨细胞中TGF-β1和TGF-β2的表达。 |
| Synonyms | 双醋瑞因, Diacerhein, Fisiodar, Diacetylrhein |
| molecular weight | 368.29 |
| Molecular formula | C19H12O8 |
| CAS | 13739-02-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (122.2 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Yaron M, et al. Osteoarthritis Cartilage, 1999, 7(3), 272-280. 2. Felisaz N, et al. Osteoarthritis Cartilage, 1999, 7(3), 255-264. 3. Boileau C, et al. Arthritis Res Ther, 2008, 10(3), R71. 4. Tamura T, et al. Eur J Pharmacol, 2002, 448(1), 81-87. 5. Hwa SY, et al. J Rheumatol, 2001, 28(4), 825-834. |
| Kinase | In Vitro Growth Inhibition Assay: Stock solution of Cytarabine is prepared in absolute ethanol, and serial dilutions of Cytarabine are prepared. CCRF-CEM cells are suspended in RPMI medium supplemented with 10% FBS, 0.1% gentamicin, and 1% sodium pyruvate. The cells are suspended in their respective media to give 10 mL volumes of cell suspension at a final density of 3-6 × 104 cells/mL. Appropriate volumes of Cytarabine solution are transferred to the cell suspensions, and incubation is continued for 72 hours. The cells are spun down and resuspended in fresh Cytarabine -free medium, and final cell counts are determined. The data are analyzed by sigmoidal curve fitting of the cell count versus Cytarabine concentration, and the results are expressed as the IC50 (Cytarabine concentration that inhibits cell growth to 50% of the control value). |