CAS |
No.518-17-2 |
中文名称 |
吴茱萸碱(10mM in DMSO,无菌) |
英文名称 |
Evodiamine(10mM in DMSO,Sterile) |
分子式 |
C19H17N3O |
分子量 |
303.36 |
溶解性 |
请根据自己的实验要求使用。 |
外观(性状) |
无菌溶液 |
储存条件 |
Stroe at -20℃,6 months. |
靶点 |
Others |
通路 |
Others |
背景说明 |
Evodiamine是萱草的果实中的生物碱, 具有多种生物活性,比如抗炎,抗肥胖和抗肿瘤。 |
生物活性 |
Evodiamine is an alkaloid isolated from the fruit of Evodia rutaecarpa Bentham with diverse biological activities including anti-inflammatory, anti-obesity, and antitumor.[1-3] |
In Vitro |
Evodiamine 通过诱导细胞凋亡对多种人类癌细胞系表现出细胞毒性。此外,它是一种天然的多靶点抗肿瘤分子,通过caspase 依赖和非依赖途径、鞘磷脂途径、钙/JNK信号、PI3K/Akt/caspase 和 Fas-L/NF-κB信号通路等多种分子机制发挥抗肿瘤活性[1]。 |
In Vivo |
Evodiamine 抑制达泊西汀的代谢。与对照组相比,Evodiamine 组达泊西汀的t1/2、AUC (0-∞) 和 Tmax 药代动力学参数分别显著升高 63.3%、44.8% 和50.4%。此外,Evodiamine 显著降低去甲基达泊西汀的 t1/2 药代动力学参数和 AUC (0-∞)[2]。Evodiamine 抑制皮下 H22 异种移植模型中的肿瘤生长。Evodiamine 在体内减弱 VEGF 诱导的血管生成[3]。 |
细胞实验 |
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]. |
动物实验 |
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]. |
数据来源文献 |
[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. |
规格 |
1ml |
单位 |
瓶 |