- 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
- 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。
- 去氢钩藤碱具有镇静、保护脑神经细胞 降压的作用。
- 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。
