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Studies on the structure-activity relationship of caffeate derivatives as neuroprotective agents
Authors:Bolin Wu  Yameng Hao  Ying Chen  Qian Liu  Chao Tian  Zhili Zhang  Junyi Liu  Xiaowei Wang
Abstract:In the present study, novel ester derivatives of CAPE were designed and synthesized as neuroprotective agents. The anti-inflammatory and antioxidant activities of these compounds were evaluated at the cellular level, while the blood-brain barrier (BBB) permeability was predicted by parallel artificial membrane permeability assay (PAMPA). The results revealed that phenolic hydroxyl groups and double bonds in the structure of CAPE had important effects on neuroprotective activities. Accordingly,a preliminary structure-activity relationship was summarized in this paper. In addition, we observed a significant improvement on BBB permeability. These results provided important references for the structural modification and optimization of CAPE in the future.
Keywords:Caffeic acid phenethyl esters  Neuroprotective activity  Anti-inflammation  Anti-oxidation  BBB permeability  
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