Diacerein是一种口服有效的蒽醌类化合物，对软骨和滑膜具有抗炎、抗分解代谢和促合成代谢的特性。
Cas No.:13739-02-1
Sample solution is provided at 25 µL, 10mM.
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Diacerein is an orally active anthraquinone with anti-inflammatory, anti-catabolic, and pro-anabolic properties on cartilage and synovial membrane [1]. Diacerein can decrease the activation of IL-1β via a reduced production of IL-1 converting enzyme, as well as affect the sensitivity to IL-1 by decreasing IL-1 receptor levels on the cell surface of chondrocytes [2]. Diacerein has been widely used to alleviate osteoarthritis and inhibit SARS-CoV virus infection [3].
In vitro, Diacerein treatment for 48 hours significantly inhibited the production of TNF-α, IL-6 and IL-1β in RAW264.7 cells, with IC50 values of 126.77, 106.90, and 65.41µM, respectively[4]. Diacerein treatment for 48 hours significantly inhibited HCT116 cells, RKO cells, and SW80 cells, with IC50 values of 46.56µM, 29.93µM, and 33.47µM, respectively[5]. Treatment with 100µM Diacerein for 48 hours resulted in G2/M phase arrest of SW-1353 cells and a decrease in the mRNA levels of Cyclin B1, CDK1, and CDK2[6].
In vivo, Diacerein treatment via intravenous tail vein injection at a dose of 40 mg/kg every other day for 4 weeks significantly inhibited tumor growth in the MDA-MB-231 xenograft mouse model and led to reduced phosphorylation levels of STAT3, MAPK, and Akt in the tumors [7]. Oral administration of 100mg/kg/day Diacerein for 21 days significantly prevented bone loss, reduced the serum alkaline phosphatase, and decreased the excretion of urinary hydroxyproline in the ovariectomized rats[8].
References:
[1] Pavelka K, Bruyere O, Cooper C, et al. Diacerein: benefits, risks and place in the management of osteoarthritis. An opinion-based report from the ESCEO[J]. Drugs & aging, 2016, 33(2): 75-85.
[2] Almezgagi M, Zhang Y, Hezam K, et al. Diacerein: Recent insight into pharmacological activities and molecular pathways[J]. Biomedicine & Pharmacotherapy, 2020, 131: 110594.
[3] de Oliveira P G, Termini L, Durigon E L, et al. Diacerein: A potential multi-target therapeutic drug for COVID-19[J]. Medical hypotheses, 2020, 144: 109920.
[4] Wang J, Wei W, Zhang X, et al. Synthesis and biological evaluation of C-17-amino-substituted pyrazole-fused betulinic acid derivatives as novel agents for osteoarthritis treatment[J]. Journal of Medicinal Chemistry, 2021, 64(18): 13676-13692.
[5] Qiaobei Y E, Yu Z H U, Meng S H I, et al. Repurposing diacerein to suppress colorectal cancer growth by inhibiting the DCLK1/STAT3 signaling pathway[J]. Chinese Journal of Natural Medicines, 2024, 22(4): 318-328.
[6] Lohberger B, Leithner A, Stuendl N, et al. Diacerein retards cell growth of chondrosarcoma cells at the G2/M cell cycle checkpoint via cyclin B1/CDK1 and CDK2 downregulation[J]. BMC cancer, 2015, 15(1): 891.
[7] Bharti R, Dey G, Ojha P K, et al. Diacerein-mediated inhibition of IL-6/IL-6R signaling induces apoptotic effects on breast cancer[J]. Oncogene, 2016, 35(30): 3965-3975.
[8] Tamura T, Shirai T, Kosaka N, et al. Pharmacological studies of diacerein in animal models of inflammation, arthritis and bone resorption[J]. European journal of pharmacology, 2002, 448(1): 81-87.
Diacerein是一种口服有效的蒽醌类化合物，对软骨和滑膜具有抗炎、抗分解代谢和促合成代谢的特性[1]。Diacerein可通过减少IL-1转化酶的产生来降低IL-1β的激活，并通过降低软骨细胞表面IL-1受体的水平来影响细胞对IL-1的敏感性[2]。Diacerein已被广泛用于缓解骨关节炎和抑制SARS-CoV病毒感染[3]。
在体外，Diacerein处理RAW264.7细胞48小时，显著抑制了TNF-α、IL-6和IL-1β的产生，IC50值分别为126.77、106.90和65.41µM[4]。Diacerein处理HCT116细胞、RKO细胞和SW80细胞48小时，显著抑制了细胞增殖，IC50值分别为46.56µM、29.93µM和33.47µM[5]。100µM的Diacerein处理SW-1353细胞48小时，导致细胞周期阻滞在G2/M期，并降低了Cyclin B1、CDK1和CDK2的mRNA水平[6]。
在体内，隔日尾静脉注射40mg/kg剂量的Diacerein，持续4周，显著抑制了MDA-MB-231异种移植小鼠模型中的肿瘤生长，并导致肿瘤中STAT3、MAPK和Akt的磷酸化水平降低[7]。每日口服100mg/kg剂量的Diacerein，持续21天，显著预防了去卵巢大鼠的骨丢失，降低了血清碱性磷酸酶水平，并减少了尿羟脯氨酸的排泄[8]。
| Cell experiment [1]: | |
Cell lines | HCT116 cells |
Preparation Method | HCT116 cells were grown in RPMI-1640 medium with 10% (v/v) fetal bovine serum (FBS), antibiotic/antimycotic solution at 37°C in 5% CO2/atmosphere. Cells were seeded in 96-well plates at a density of 5×103 cells and cultured overnight. After 48h of treatment with different concentrations of Diacerein (0, 1, 10, 20, 40, 60, 80, and 100µM), the cell viability was measured. |
Reaction Conditions | 0, 1, 10, 20, 40, 60, 80, and 100µM; 48h |
Applications | Diacerein treatment significantly inhibited the cell viability of HCT116 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female nude athymic mice |
Preparation Method | Female nude athymic mice (6 weeks old; 22-25g) were housed singly in a standard environment with food and water ad libitum. MDA-MB-231 cells (5×106 cells) were injected into female mice subcutaneously. After 12 days, tumors developed, and the mice were randomly divided into three groups. The treatment (via tail vein) regimens were as follows: (1) control group, (2) Diacerein (40mg/kg; i.v.). Each group contained five mice. Mice were treated for 4 weeks in alternative days. During the treatment, visible toxicity and a change in body weight were observed. At the end of the experiment, mice were killed, and tumor volume and weight were measured. |
Dosage form | 40mg/kg; alternative days for 4 weeks; i.v. |
Applications | Diacerein treatment significantly reduced the development of MDA-MB-231 xenograft tumors in mice. |
References: | |
| Cas No. | 13739-02-1 | SDF | |
| 别名 | 双醋瑞因; Diacerhein; Diacetylrhein | ||
| 化学名 | 4,5-diacetyloxy-9,10-dioxoanthracene-2-carboxylic acid | ||
| Canonical SMILES | CC(=O)OC1=CC=CC2=C1C(=O)C3=C(C=C(C=C3C2=O)C(=O)O)OC(=O)C | ||
| 分子式 | C19H12O8 | 分子量 | 368.29 |
| 溶解度 | ≥ 46.07mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7153 mL | 13.5763 mL | 27.1525 mL |
| 5 mM | 543.1 μL | 2.7153 mL | 5.4305 mL |
| 10 mM | 271.5 μL | 1.3576 mL | 2.7153 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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- Purity: >98.50% Appearance: A solid
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