Evodiamine
(Synonyms: (±)-吴茱萸碱) 目录号 : GN10048
A natural alkaloid with therapeutic actions
Cas No.:518-17-2
Sample solution is provided at 25 µL, 10mM.
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Evodiamine is an alkaloid isolated from the fruit of Evodia rutaecarpa Bentham with diverse biological activities including anti-inflammatory, anti-obesity, and antitumor.
Evodiamine shows cytotoxicity against a variety of human cancer cell-lines by inducing apoptosis. Moreover, it is a naturally multi-targeting antitumor molecule, which exerts the antitumor activity by various molecular mechanism such as caspase-dependent and -independent pathways, sphingomyelin pathway, calcium/JNK signaling, 31 PI3K/Akt/caspase and Fas-L/NF-κB signaling pathways32[1].
Evodiamine inhibits the metabolism of dapoxetine. Compared to the control group, the pharmacokinetic parameter of t1/2, AUC(0-∞) and Tmax of dapoxetine in evodiamine group is significantly increased by 63.3%, 44.8% and 50.4%, respectively. Moreover, evodiamine has significantly decreased the pharmacokinetic parameter of t1/2 and AUC(0-∞) of desmethyl dapoxetine[2]. Evodiamine suppresses tumor growth in a subcutaneous H22 xenograft model. Evodiamine attenuates VEGF-induced angiogenesis in vivo[3].
References:
[1]. Wang S, et al. Scaffold Diversity Inspired by the Natural Product Evodiamine: Discovery of Highly Potent and Multitargeting Antitumor Agents. J Med Chem. 2015 Aug 27;58(16):6678-96.
[2]. Li RF,et al. Effects of Evodiamine on the Pharmacokinetics of Dapoxetine and Its Metabolite Desmethyl Dapoxetine inRats. Pharmacology. 2016;97(1-2):43-7.
[3]. Shi L, et al. Evodiamine exerts anti-tumor effects against hepatocellular carcinoma through inhibiting β-catenin-mediated angiogenesis. Tumour Biol. 2016 Sep;37(9):12791-12803.
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Cell experiment: |
Evodiamine is dissolved in DMSO and diluted with appropriate medium before use. The evodiamine-inspired new scaffolds are assayed for growth inhibitory activities toward human cancer cell-lines A549 (lung cancer), MDA-MB-435 (breast cancer) and HCT116 (colon cancer) using the MTT assay. Evodiamine and camptithecin are used as reference drugs[1]. |
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Animal experiment: |
Rats: Twelve healthy male Sprague-Dawley rats are randomly divided into 2 groups: the control group (received oral 10 mg/kg dapoxetine alone) and the combination group (10 mg/kg dapoxetine orally co-administered with 100 mg/kg evodiamine). The plasma concentration of dapoxetine and desmethyl dapoxetine are estimated by ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS), and different pharmacokinetic parameters are calculated[2]. Mice: A nude mouse xenograft model is established by using 4–6-week-old male BALB/c nude mice. Mice are dosed daily with 20 mg/kg (10 mL/kg) of evodiamine intragastrically, six mice are dosed intraperitoneally with 10 mg/kg of 5-flurouracil (5-FU) twice a week, and six mice are not treated. The tumor volumes are determined by measuring two dimensions, with tumor volume=length×width×width/2. After 2 or 3 weeks of treatment, mice are sacrificed by cervical dislocation under anesthesia with ether, and the tumor tissues are collected[3]. |
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References: [1]. Wang S, et al. Scaffold Diversity Inspired by the Natural Product Evodiamine: Discovery of Highly Potent and Multitargeting Antitumor Agents. J Med Chem. 2015 Aug 27;58(16):6678-96. |
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| Cas No. | 518-17-2 | SDF | |
| 别名 | (±)-吴茱萸碱 | ||
| 化学名 | (S)-14-methyl-7,8,13b,14-tetrahydroindolo[2',3':3,4]pyrido[2,1-b]quinazolin-5(13H)-one | ||
| Canonical SMILES | O=C1N2[C@](C(N([H])C3=C([H])C([H])=C([H])C([H])=C43)=C4C([H])([H])C2([H])[H])([H])N(C([H])([H])[H])C5=C([H])C([H])=C([H])C([H])=C15 | ||
| 分子式 | C19H17N3O | 分子量 | 303.35 |
| 溶解度 | ≥ 30.3mg/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 | 3.2965 mL | 16.4826 mL | 32.9652 mL |
| 5 mM | 0.6593 mL | 3.2965 mL | 6.593 mL |
| 10 mM | 0.3297 mL | 1.6483 mL | 3.2965 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet