Journal of Chinese Pharmaceutical Sciences

• Original articles • Previous Articles     Next Articles

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

Renzong Zhu, Xianling Ning, Zhili Zhang, Xiaowei Wang, Chao Tian, Junyi Liu*   

  1. Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2013-06-03 Revised:2013-06-15 Online:2013-11-15 Published:2014-01-22
  • Contact: Junyi Liu*


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 H2O2 model and 6-OHDA model. The results showed that target compounds displayed positive abilities to protect PC12 nerve cells from oxidative stress injury, superior to that of CAPE. Additionally, target compounds showed high blood-brain barrier permeability.

Key words: Amyotrophic lateral sclerosis, Acylation, Caffeic acid phenethyl ester, Neuroprotective agents, Blood-brain barrier permeability

CLC Number: