Rhein

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Chemical Structure| 478-43-3 同义名 : Rheic Acid;Rhubarb yellow;Rheic acid, Cassic acid;Rheinic Acid;NSC 38629;Monorhein
CAS号 : 478-43-3
货号 : A105483
分子式 : C15H8O6
纯度 : 98+%
分子量 : 284.22
MDL号 : MFCD00009618
存储条件：

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(42.22 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

0.1 M NaOH: 10 mg/mL(35.18 mM)
动物实验配方：
生物活性
描述 Rhein is a lipophilic anthraquinone extensively found in medicinal herbs. Apoptosis was induced by adjunctive use of rhein with epidermal growth factor receptor (EGFR) inhibitors in pancreatic cancer cells. Suppression of the phosphorylation of STAT3 and EGFR (epidermal growth factor receptor) were also observed as a result of the treatment with a combination of rhein and EGFR inhibitors. Rhein considerably sensitized cells to erlotinib, thus suppressing tumor growth in PANC-1 and BxPC-3 xenograft models[3]. Rhein possesses pharmacological activity to suppress caspase-1 protease activity and IL-1 βproduction by interfering with the formation of NLRP3 multiprotein complex. Rhein has therapeutic potential for treating NLRP3 inflammasome-mediated diseases such as gouty arthritis[4]. Rhein exhibits various renoprotective functions, rhein remarkably reversed renal Klotho (a renal-specific antiaging protein) deficiency in adenine-treated mice. The renal protective effects of rhein were largely abolished when Klotho was knocked-down by RNA interferences, suggesting that rhein reversal of Klotho deficiency is essential for its renoprotective actions[5]. Rhein could effectively block the ATP-induced [Ca2+]c increases in a dose-dependent manner. Besides, rhein also suppressed the production of intracellular reactive oxygen species (ROS) induced by ATP in synoviocytes that was resulted from P2X4-mediated Ca2+ entry. Both rhein and BBG (Brilliant blue G) attenuated these inflammatory gene expressions enhanced by ATP[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.52mL

0.70mL

0.35mL

17.59mL

3.52mL

1.76mL

35.18mL

7.04mL

3.52mL
参考文献

[1]Lin S, Fujii M, Hou DX. Rhein induces apoptosis in HL-60 cells via reactive oxygen species-independent mitochondrial death pathway. Arch Biochem Biophys. 2003 Oct 15;418(2):99-107.

[2]Martel-Pelletier J, Mineau F, et al. In vitro effects of diacerhein and rhein on interleukin 1 and tumor necrosis factor-alpha systems in human osteoarthritic synovium and chondrocytes. J Rheumatol. 1998 Apr;25(4):753-62.

[3]Yang L, Lin S, Kang Y, et al. Rhein sensitizes human pancreatic cancer cells to EGFR inhibitors by inhibiting STAT3 pathway. J Exp Clin Cancer Res. 2019;38(1):31. Published 2019 Jan 23

[4]Chang WC, Chu MT, Hsu CY, et al. Rhein, An Anthraquinone Drug, Suppresses the NLRP3 Inflammasome and Macrophage Activation in Urate Crystal-Induced Gouty Inflammation. Am J Chin Med. 2019;47(1):135-151

[5]Zhang Q, Liu L, Lin W, et al. Rhein reverses Klotho repression via promoter demethylation and protects against kidney and bone injuries in mice with chronic kidney disease. Kidney Int. 2017;91(1):144-156

[6]Hu F, Zhu D, Pei W, et al. Rhein inhibits ATP-triggered inflammatory responses in rheumatoid rat fibroblast-like synoviocytes. Int Immunopharmacol. 2019;75:105780