去氢钩藤碱

中文名称:

去氢钩藤碱

中文同义词:

CORYNOXEINE 去氢钩藤碱;柯诺辛因碱;去氢钩藤碱(标准品);去氢钩藤碱(柯诺辛因碱);去氢钩藤碱;去氢钩藤碱?, 99.9%;ERK1/2抑制剂(CORYNOXEINE)

英文名称:

corynoxeine

英文同义词:

corynoxeine;(7R,16E,20α)-16,17,18,19-Tetradehydro-17-methoxy-2-oxocorynoxan-16-carboxylic acid methyl ester;(alphaE,1R,6R,7S,8aS)-6-Ethenyl-1,2,2,3,6,7,8,8a-octahydro-alpha-(methoxymethylene)-2-oxospiro[3H-indole-3,1(5H)-indolizine]-7-acetic acid methyl ester;16,17,18,19-Tetradehydro-17-methoxy-2-oxocorynoxan-16-carboxylic acid methyl ester;Spiro[3H-indole-3,1(5H)-indolizine]-7-aceticacid, 6-ethenyl-1,2,2,3,6,7,8,8a-octahydro-a-(methoxymethylene)-2-oxo-, methyl ester, (aE,1R,6R,7S,8aS)-;Corynoxeine, 99.9%;Spiro[3H-indole-3,1(5H)-indolizine]-7-acetic acid, 6-ethenyl-1,2,2,3,6,7,8,8a-octahydro-α-(methoxymethylene)-2-oxo-, methyl ester, (αE,1R,6R,7S,8aS)-;corynoxeine USP/EP/BP

CAS号:

630-94-4

分子式:

C22H26N2O4

分子量:

382.46

EINECS号:

相关类别:

中药对照品;标准品;对照品,标准品;植物提取物;中草药成分;对照品;植提标准品;chemical reagent;pharmaceutical intermediate;phytochemical;reference standards from Chinese medicinal herbs (TCM).;standardized herbal extract;分析试剂标准品;细胞生物学试剂;标准品-中药标准品;标准品 -中药标准品;标准品，对照品

Mol文件:

630-94-4.mol

熔点 

210℃

沸点 

562.7±50.0 °C(Predicted)

密度 

1.25

酸度系数(pKa)

13.54±0.60(Predicted)

应用

去氢钩藤碱对高血压大鼠主动脉环有舒张作用，具有扩张外周血管和负心心肌肌力、降血压作用，可用于制备制备扩血管药物以及降血压药物；所述的钩藤有效成分去氢钩藤碱具有扩张血管、降低心脏后负荷和降低心肌收缩力的作用，可降低心肌耗氧量，用于制备抗心绞痛药物，尤其可制备心绞痛急救的药物；所述的去氢钩藤碱具有负性肌力作用，可用于制备抗室性心动过速药物；所述的去氢钩藤碱具有提高心室肌兴奋阈值的作用，可制备抗室性心律失常药物。

制备

钩藤钩经乙酸乙酯回流提取 2 h（×3），提取物经硅胶柱分离，以及制备高效液相色谱分离纯化而得到去氢钩藤碱、异去氢钩藤碱，经与标准品的1H NMR、13CNMR 图谱对照，与标准品的 LC- MS 分子离子峰的保留时间和 m/z 对比，确证为去氢钩藤碱、异去氢钩藤碱。

生物活性

Corynoxeine, 从 Uncaria rhynchophylla 的钩中分离的，是 PDGF-BB 诱导血管平滑肌细胞 (VSMCs) 增殖过程中的一种有效 ERK1/ERK 2 抑制剂。

靶点

ERK1 ERK2

ERK1

ERK2

体外研究

Corynoxeine is able to inhibit the PDGF-BB-stimulated proliferation of VSMCs through downregulation of PDGF-BB-induced ERK1/2 activation. Pre-incubation of VSMCs with Corynoxeine significantly inhibits PDGF-BB-induced extracellular signal-regulated kinase 1/2 (ERK1/2) activation, whereas Corynoxeine has no effects on mitogen-activated protein kinase (MAPK/ERK)-activating kinase 1 and 2 (MEK1/2), Akt, or phospholipase C (PLC) γ 1 activation or on PDGF receptor beta (PDGF-Rβ) phosphorylation. Corynoxeine inhibits PDGF-BB-induced ERK1/2 activation, in the same concentration range that inhibits VSMC proliferation and DNA synthesis. Corynoxeine inhibits VSMC numbers in response to PDGF-BB with 50% inhibitory concentrations (IC 50 ) of 13.7 μM. Corynoxeine inhibits DNA synthesis in response to PDGF-BB (24 h) with IC 50 of 9.2 μM. Pre-treatment of VSMCs with Corynoxeine (5-50 μM) for 24 h results in significant decreases in cell number without any cytotoxicity; the inhibition percentages are 25.0±12.5, 63.0±27.5 and 88.0±12.5% at 5, 20 and 50 μM, respectively. Corynoxeine also significantly inhibits the 50 ng/mL PDGF-BB-induced DNA synthesis of VSMCs in a concentration-dependent manner without any cytotoxicity; the inhibitions are 32.8±11.0, 51.8±8.0 and 76.9±7.4% at concentrations of 5, 20 and 50 μM, respectively.

化学性质 

白色结晶粉末，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于钩藤。

用途 

去氢钩藤碱具有镇静、保护脑神经细胞 降压的作用。

用途 

用于含量测定/鉴定/药理实验等。 药理药效:本品有抑制呼吸中枢和离体肠管及兴奋大鼠离体子宫，降低血压，抗血小板聚集并有促进已聚集血小板解聚的作用。还能改善红细胞的变形能力，抑制不良因素对红细胞变形能力的损害。临床用于治疗高血压病，对I、II期高血压有一定的疗效。