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Rutaecarpine

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Chemical Structure| 84-26-4 同义名 : Rutecarpine;NSC 258317
CAS号 : 84-26-4
货号 : A331454
分子式 : C18H13N3O
纯度 : 95%
分子量 : 287.315
MDL号 : MFCD00210551
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(174.02 mM),配合低频超声助溶,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

动物实验配方:
生物活性
靶点
  • COX-2

描述 Rutaecarpine inhibited COX-2 and COX-1 dependent phases of PGD2 generation in BMMC in a concentration-dependent manner with an IC50 of 0.28 microM and 8.7 microM, respectively. It inhibited COX-2-dependent conversion of exogenous arachidonic acid to PGE2 in a dose-dependent manner by the COX-2-transfected HEK293 cells. However, rutaecarpine inhibited neither PLA2 and COX-1 activity nor COX-2 protein and mRNA expression up to the concentration of 30 microM in BMMC, indicating that rutaecarpine directly inhibited COX-2 activity. Furthermore, rutaecarpine showed in vivo anti-inflammatory activity on rat lambda-carrageenan induced paw edema by intraperitoneal administration[3]. Rutaecarpine is an indolopyridoquinazolinone alkaloid isolated from Evodia rutaecarpa and related herbs, which has shown a variety of intriguing biological properties such as anti-thrombotic, anticancer, anti-inflammatory and analgesic, anti-obesity and thermoregulatory, vasorelaxing activity, as well as effects on the cardiovascular and endocrine systems[4]. Rutaecarpine significantly decreased the number of antibody-forming cells and caused weight decrease in spleen in a dose-dependent manner, when mice were administered with rutaecarpine at 10 mg/kg, 20 mg/kg, 40 mg/kg or 80 mg/kg once intravenously. A single bolus intravenous injection of rutaecarpine from 20 mg/kg might cause immunosuppressive effects, and that rutaecarpine-induced immunosuppression might be mediated, at least in part, through the inhibition of cytokine production and cell cycle arrest in G(0)+G(1) phase, and caused possibly by mechanisms associated with metabolic activation[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.48mL

0.70mL

0.35mL

17.40mL

3.48mL

1.74mL

34.81mL

6.96mL

3.48mL

参考文献

[1]Lee SH, Son JK, Jeong BS, Jeong TC, Chang HW, Lee ES, Jahng Y. Progress in the studies on rutaecarpine. Molecules. 2008 Feb 6;13(2):272-300.

[2]Yang XW, Zhang H, et al. Studies on the alkaloid constituents of Evodia rutaecarpa (Juss) Benth var. bodinaieri (Dode) Huang and their acute toxicity in mice. J Asian Nat Prod Res. 2006 Dec;8(8):697-703.

[3]Moon TC, Murakami M, Kudo I, et al. A new class of COX-2 inhibitor, rutaecarpine from Evodia rutaecarpa. Inflamm Res. 1999;48(12):621-625

[4]Lee SH, Son JK, Jeong BS, et al. Progress in the studies on rutaecarpine. Molecules. 2008;13(2):272-300. Published 2008 Feb 6

[5]Jeon TW, Jin CH, Lee SK, et al. Immunosuppressive effects of rutaecarpine in female BALB/c mice. Toxicol Lett. 2006;164(2):155-166