earticle

영어

In this study, eight kinds of phenolic acid conjugated COSs were synthesized from benzoic acid and cinnamic acid. Eight kinds of chitooligosaccharides (COS) with different substitution groups, including p-hydroxyl (HBA-COS, PCA-COS), 3,4-dihydroxyl (PTA-COS, CFA-COS), 3-methoxyl-4-hydroxyl (VNA-COS, FRA-COS) and 3,5-dimethoxyl- 4-hydroxy (SRA-COS, SNA-COS) groups, were evaluated for their inhibitory activities against β-Secretase (BACE). Cinnamic acid derivatives showed the strongest BACE inhibitory activity more than benzoic acid derivatives. In addition, catechol structure substantially increased the BACE inhibitory activity of the COS derivatives. CFA-COS was further analyzed for its inhibitory pattern on BACE via Lineweaver–urk plots. CFA-COS showed non-competitive inhibition of BACE. In this study, we suggested that phenolic acid conjugated COS derivatives have potential as BACE inhibitors for preventing Alzheimer’ disease.