期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 20, 页码 6498-6502出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.08.036
关键词
Caffeic acid; Dimer; Alzheimer's disease; Antioxidants; Acetylcholinesterase; Multi-targeted compounds
资金
- Fundamental Research Funds for the Central Universities [10ykpy23]
- Guangdong Provincial International Cooperation Project of Science Technology [2012B050300015]
- National Natural Science Foundation of China/RGC Hong Kong Joint Research Scheme [30731160617]
A novel series of tacrine-caffeic acid hybrids (5a-f) were designed and synthesized by combining caffeic acid (CA) with tacrine. The antioxidant study revealed that all the hybrids have much more antioxidant capacities compared to CA. Among these compounds, 5e showed the highest selectivity in inhibiting acetylcholinesterase (AChE) over butyrylcholinesterase (BuChE). Enzyme kinetic study had suggested that 5e binds to both catalytic (CAS) and peripheral anionic sites (PAS) of AChE. Moreover, compound 5e also inhibited self- or AChE-induced beta-amyloid(1-40) aggregation, as well as had potent neuroprotective effects against H2O2- and glutamate- induced cell death with low toxicity in HT22 cells. (c) 2012 Elsevier Ltd. All rights reserved.
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