Eight kinds of phenolic acid conjugated chitooligosaccharides (COSs) were synthesized using hydroxyl benzoic acid and hydroxyl cinnamic acid. These phenolic acid conjugated-COSs with different substitution groups, including p-hydroxyl, 3,4-dihydroxyl, 3-methoxyl-4-hydroxyl and 3,5-dimethoxyl-4-hydroxy groups, were evaluated for their inhibitory activities against β-site amyloid precursor protein (APP)-cleaving enzyme (BACE) and inhibited BACE with a ratio of 50.8%, 74.8%, 62.1%, 64.8% and 42.6%, respectively at the concentration of 1,000 μg/mL. BACE is a critical component to reduce the levels of Aβ amyloid peptide in Alzheimer’s disease (AD) which is based on the amyloid cascade theory in the brain, as this protease initiates the first step in Aβ production. Among them, Caffeic acid conjugated-COS (CFA-COS) was further analysed to determine mode of inhibition of BACE and it showed non-competitive inhibition. Hence in this study, we suggest that CFA-COS derivatives have potential to be used as novel BACE inhibitors to reduce the risk of AD.

Tae-Kil Eom

BoMi Ryu

Jung-Kwon Lee

Hee-Guk Byun

Sun-Joo Park

Se-Kwon Kim

Journal of Enzyme Inhibition and Medicinal Chemistry

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 发表关于药物和抗癌药物开发中酶抑制剂、抑制过程和激动剂/拮抗剂受体相互作用的开放获取研究。JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 旨在提供一个国际化和跨学科的平台获取酶抑制研究的最新发现。该杂志的重点包括以下领域的最新发展：酶学；细胞生物学；化学生物学；微生物学；生理学；导致药物设计的药理学；分子识别过程；生物活性化合物的分布和代谢。

The Journal of Enzyme Inhibition and Medicinal Chemistry publishes open-access research on enzyme inhibitors, inhibition processes, and agonist/antagonist receptor interactions in the development of drugs and anticancer agents. The journal aims to provide an international and interdisciplinary platform for accessing the latest findings in enzyme inhibition research. Key areas of focus include recent developments in enzymology, cell biology, chemical biology, microbiology, physiology, pharmacology related to drug design, molecular recognition processes, and the distribution and metabolism of bioactive compounds.

《Journal of Enzyme Inhibition and Medicinal Chemistry》发表关于药物和抗癌药物开发中酶抑制剂、抑制过程及激动剂/拮抗剂受体相互作用的开放获取研究。该期刊旨在提供一个国际化和跨学科的平台，以获取酶抑制研究的最新发现。重点领域包括：酶学、细胞生物学、化学生物学、微生物学、生理学、药理学（尤其是药物设计相关）、分子识别过程，以及生物活性化合物的分布和代谢。

β-secretase inhibitory activity of phenolic acid conjugated chitooligosaccharides

It is suggested that CFA-COS derivatives have potential to be used as novel BACE inhibitors to reduce the risk of AD.

Category	Quartile
医学	2
医学, 生化与分子生物学	2
医学, 药物化学	2

β-secretase inhibitory activity of phenolic acid conjugated chitooligosaccharides

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