去氢钩藤碱 用途与合成方法 |
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 |
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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.
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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。 |
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