Studies on the structure-activity relationship of caffeate derivatives as neuroprotective agents

doi:10.5246/jcps.2019.09.059

Abstract

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.

Key words: Caffeic acid phenethyl esters, Neuroprotective activity, Anti-inflammation, Anti-oxidation, BBB permeability

CLC Number:

R914

Supporting:

Bolin Wu, Yameng Hao, Ying Chen, Qian Liu, Chao Tian, Zhili Zhang, Junyi Liu, Xiaowei Wang. Studies on the structure-activity relationship of caffeate derivatives as neuroprotective agents[J]. Journal of Chinese Pharmaceutical Sciences, 2019, 28(9): 615-626.

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