Design, synthesis and pharmacological evaluation of caffeic acid phenethyl ester acylation as multifunctional neuroprotective agents against oxidative stress injury

咖啡酸苯乙酯酰化衍生物的设计、合成及其作为抗氧化应激损伤的中枢神经保护剂的活性评估(英文)

4-Acylated or 3,4-diacylated caffeic acid phenethyl ester （CAPE） was prepared as prodrug to improve its stability and lipid solubility. Their neuroprotective activities were assessed by H202 model and 6-OHDA model. The results showed that target compounds displayed positive abilities to protect PC 12 nerve cells from oxidative stress injury, superior to that of CAPE. Additionally, target compounds showed high blood-brain barrier permeability.

以咖啡酸苯乙酯(CAPE)为先导物,将其对位酚羟基或间位、对位两个酚羟基进行酰化,制备CAPE的前药,提高其稳定性和脂溶性。并采用了H2O2和6-OHDA两种模型对其进行了神经保护活性测定。结果显示目标化合物相较于CAPE能够更好地保护PC12神经细胞免受氧化应激损伤。此外,目标化合物也显示出了较强的血脑屏障透过能力。