(±)-Evodiamine, a quinazolinocarboline alkaloid, is a Top1 inhibitor. Evodiamine exhibits anti-inflammatory, antiobesity, and antitumor effects. (±)-Evodiamine inhibits the proliferation of a wide variety of tumor cells by inducing their apoptosis[1].
IC50 & Target[1]
Top1
分子量
303.36
Formula
C19H17N3O
CAS 号
518-18-3
中文名称
(±)-吴茱萸碱
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 10 mg/mL (32.96 mM; ultrasonic and warming and heat to 60°C)
[1]. Dong G, et, al. New tricks for an old natural product: discovery of highly potent evodiamine derivatives as novel antitumor agents by systemic structure-activity relationship analysis and biological evaluations. J Med Chem. 2012 Sep 13;55(17):7593-613.
(±)-Evodiamine, a quinazolinocarboline alkaloid, is a Top1 inhibitor. Evodiamine exhibits anti-inflammatory, antiobesity, and antitumor effects. (±)-Evodiamine inhibits the proliferation of a wide variety of tumor cells by inducing their apoptosis[1].
IC50 & Target[1]
Top1
分子量
303.36
Formula
C19H17N3O
CAS 号
518-18-3
中文名称
(±)-吴茱萸碱
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 10 mg/mL (32.96 mM; ultrasonic and warming and heat to 60°C)
[1]. Dong G, et, al. New tricks for an old natural product: discovery of highly potent evodiamine derivatives as novel antitumor agents by systemic structure-activity relationship analysis and biological evaluations. J Med Chem. 2012 Sep 13;55(17):7593-613.
(±)-Evodiamine, a quinazolinocarboline alkaloid, is a Top1 inhibitor. Evodiamine exhibits anti-inflammatory, antiobesity, and antitumor effects. (±)-Evodiamine inhibits the proliferation of a wide variety of tumor cells by inducing their apoptosis[1].
IC50 & Target[1]
Top1
分子量
303.36
Formula
C19H17N3O
CAS 号
518-18-3
中文名称
(±)-吴茱萸碱
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 10 mg/mL (32.96 mM; ultrasonic and warming and heat to 60°C)
[1]. Dong G, et, al. New tricks for an old natural product: discovery of highly potent evodiamine derivatives as novel antitumor agents by systemic structure-activity relationship analysis and biological evaluations. J Med Chem. 2012 Sep 13;55(17):7593-613.
Evodiamine is an alkaloid isolated from the fruit of Evodia rutaecarpa Bentham with diverse biological activities including anti-inflammatory, anti-obesity, and antitumor.
体外研究 (In Vitro)
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].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
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].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
303.36
Formula
C19H17N3O
CAS 号
518-17-2
中文名称
吴茱萸碱;吴茱萸胺
运输条件
Room temperature in continental US; may vary elsewhere.
[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.
Cell Assay [1]
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].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [2][3]
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].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[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.