Rutaecarpine
(Synonyms: 吴茱萸次碱; Rutecarpine) 目录号 : GN10039
Rutaecarpine是一种从吴茱萸中分离出的吲哚并吡啶喹唑啉生物碱，已知在细胞水平上以0.28μM的IC50抑制COX-2。
Cas No.:84-26-4
Sample solution is provided at 25 µL, 10mM.
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Rutaecarpine is an indolopyridoquinazoline alkaloid isolated from Evodia rutaecarpa and known to inhibit COX-2 with an IC50 of 0.28μM at the cellular level[1]. Rutaecarpine exhibits various pharmacological effects, such as anti‑inflammatory[2], anti‑apoptotic and antioxidant effects[3]. Rutaecarpine plays critical roles in cardiovascular[4], nervous system, inflammatory and tumor diseases[5].
Rutaecarpine at concentrations of 10µM for 24h effectively attenuated IL‑1β‑induced chondrocyte apoptosis, senescence and autophagy impairment in chondrocytes[6]. In HepG2 cells, Rutaecarpine at concentrations of 40µM for 24h increases p-GSK-3b and p-AMPK, and decreased G6Pase expression[7].
Rutaecarpine (20mg/kg, intragastric administration, daily for 9 days) inhibited oxidative stress in NTG-induced mice and improves migraine by activation of the Nrf2 antioxidant system through the PTEN/PGK1 pathway[8]. Rutaecarpine (10mg/kg, 20mg/kg, 40mg/kg) significantly decreased the number of antibody-forming cells and caused weight decrease in mouse spleen in a dose-dependent manner[9].
References:
[1]. Moon TC, Murakami M, Kudo I, et al. A new class of COX-2 inhibitor, rutaecarpine from Evodia rutaecarpa. Inflamm Res. 1999 Dec;48(12):621-5. doi: 10.1007/s000110050512. PMID: 10669112.
[2]. Jayakumar T, Lin KC, Chang CC, et al. Targeting MAPK/NF-κB Pathways in Anti-Inflammatory Potential of Rutaecarpine: Impact on Src/FAK-Mediated Macrophage Migration. Int J Mol Sci. 2021 Dec 22;23(1):92. doi: 10.3390/ijms23010092. PMID: 35008520; PMCID: PMC8745017.
[3]. Choi JH, Jin SW, Lee GH, et al. Rutaecarpine Protects against Acetaminophen-Induced Acute Liver Injury in Mice by Activating Antioxidant Enzymes. Antioxidants (Basel). 2021 Jan 10;10(1):86. doi: 10.3390/antiox10010086. PMID: 33435214; PMCID: PMC7827407.
[4]. Jia S, Hu C. Pharmacological effects of rutaecarpine as a cardiovascular protective agent. Molecules. 2010 Mar 15;15(3):1873-81. doi: 10.3390/molecules15031873. PMID: 20336017; PMCID: PMC6257227.
[5]. Chan S, Sun R, Tu X, et al. Rutaecarpine suppresses the proliferation and metastasis of colon cancer cells by regulating the STAT3 signaling. J Cancer. 2022 Jan 1;13(3):847-857. doi: 10.7150/jca.66177. PMID: 35154453; PMCID: PMC8824880.
[6]. Wan J, Li M, Yuan X, et al. Rutaecarpine ameliorates osteoarthritis by inhibiting PI3K/AKT/NF‑κB and MAPK signalling transduction through integrin αVβ3. Int J Mol Med. 2023 Oct;52(4):97. doi: 10.3892/ijmm.2023.5300. Epub 2023 Sep 1. PMID: 37654229; PMCID: PMC10555473.
[7]. Surbala L, Singh CB, Devi RV, et al. Rutaecarpine exhibits anti-diabetic potential in high fat diet-multiple low dose streptozotocin induced type 2 diabetic mice and in vitro by modulating hepatic glucose homeostasis. J Pharmacol Sci. 2020 Aug;143(4):307-314. doi: 10.1016/j.jphs.2020.04.008. Epub 2020 Jun 9. PMID: 32536591.
[8]. Xu M, Shi Z, He Z, et al. Rutaecarpine alleviates migraine in nitroglycerin-induced mice by regulating PTEN/PGK1 signaling pathway to activate NRF2 antioxidant system. Biomed Pharmacother. 2023 Oct;166:115300. doi: 10.1016/j.biopha.2023.115300. Epub 2023 Aug 7. PMID: 37557014.
[9]. Jeon TW, Jin CH, Lee SK, et al. Immunosuppressive effects of rutaecarpine in female BALB/c mice. Toxicol Lett. 2006 Jul 1;164(2):155-66. doi: 10.1016/j.toxlet.2005.12.005. Epub 2006 Jan 18. PMID: 16412592.
Rutaecarpine是一种从吴茱萸中分离出的吲哚并吡啶喹唑啉生物碱，已知在细胞水平上以0.28μM的IC50抑制COX-2[1]。Rutaecarpine表现出多种药理作用，如抗炎[2]、抗凋亡和抗氧化作用[3]。Rutaecarpine在心血管[4]、神经系统、炎症和肿瘤疾病中发挥关键作用[5]。
Rutaecarpine (10µM) 处理24小时有效减轻了IL-1β诱导的软骨细胞凋亡、衰老和自噬障碍[6]。在HepG2细胞中，40µM浓度的Rutaecarpine处理24小时增加了p-GSK-3β和p-AMPK的表达，并降低了G6Pase的表达[7]。
Rutaecarpine（20mg/kg，灌胃，每日一次，连续9天）在NTG诱导的小鼠中抑制了氧化应激，并通过PTEN/PGK1通路激活Nrf2抗氧化系统，从而改善偏头痛[8]。Rutaecarpine处理（10mg/kg、20mg/kg、40mg/kg）显著减少了抗体形成细胞的数量，并以剂量依赖性方式导致小鼠脾脏重量减少[9]。
| Cell experiment [1]: | |
Cell lines | Mouse chondrocytes |
Preparation Method | Mouse chondrocytes were exposed to IL‑1β (5ng/ml) with Rutaecarpine (1, 2.5, 5 and 10µM) for 24h, then the protein expression levels of MMP3, MMP13, IL‑1β, COX2, IL‑6, TNF‑α, SOX9, COL II and aggrecan were determined using western blot analysis. |
Reaction Conditions | 1, 2.5, 5 and 10µM, 24 hours |
Applications | Rutaecarpine attenuates the IL‑1β‑induced expression of inflammatory cytokines (COX2, IL‑6, TNF‑α and IL‑1β) in a concentration-dependent manner in mouse chondrocytes. |
| Animal experiment [2]: | |
Animal models | Chronic migraine Mouse |
Preparation Method | Chronic migraine (CM) were treatment with Rutaecarpine (5, 10, 20mg/kg) and then markers associated with oxidative stress were examined by biochemical kits in the trigeminal nucleus caudalis. |
Dosage form | 5, 10, 20mg/kg/d, 9 days, i.g. |
| Rutaecarpine treatment improved NTG-induced migraine in mice by inhibiting oxidative stress. | |
References: | |
| Cas No. | 84-26-4 | SDF | |
| 别名 | 吴茱萸次碱; Rutecarpine | ||
| 化学名 | 7,8-dihydroindolo[2',3':3,4]pyrido[2,1-b]quinazolin-5(13H)-one | ||
| Canonical SMILES | O=C1N(C2=NC3=C([H])C([H])=C([H])C([H])=C13)C([H])([H])C([H])([H])C4=C2N([H])C5=C([H])C([H])=C([H])C([H])=C45 | ||
| 分子式 | C18H13N3O | 分子量 | 287.32 |
| 溶解度 | DMF: 33 mg/ml,DMSO: 12 mg/ml | 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 | 3.4804 mL | 17.4022 mL | 34.8044 mL |
| 5 mM | 0.6961 mL | 3.4804 mL | 6.9609 mL |
| 10 mM | 0.348 mL | 1.7402 mL | 3.4804 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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