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乙酰胆碱
Small · 2018 ·Vol. 14 ·期 31 ·1801680 · IF 9.598

Ag+-Gated Surface Chemistry of Gold Nanoparticles and Colorimetric Detection of Acetylcholinesterase

Jiangjiang Zhang,Wenshu Zheng,Xingyu Jiang

Chemical regulation of enzyme-mimic activity of nanomaterials is challenging because it requires a precise understanding of the surface chemistry and mechanism, and rationally designed applications. Herein, Ag + -gated peroxidase activity is demonstrated by successfully modulating surface chemistry of cetyltrimethylammonium bromide-capped gold nanoparticles (CTAB-AuNPs). A surface blocking effect of long-chain molecules on surfaces of AuNPs that inhibit peroxidase activity of AuNPs is found. Ag + ions can selectively bind on the surfaces of AuNPs and competitively destroy CTAB membrane forming Ag + @CTAB-AuNPs complexes to result in enhanced peroxidase activity. Ag + @CTAB-AuNPs show the highest peroxidase activity compared to similar-sized citrate-capped and ascorbic acid-capped AuNPs. Ag + @CTAB-AuNPs can potentially develop into analyte-responsive systems and exhibit advantages in the optical sensing field. For example, the Ag + @CTAB-AuNPs system shows an enhanced sensitivity and selectivity for acetylcholinesterase activity sensing compared to other methods.

研究领域: 纳米生物技术 · 分析化学 · 酶学 · 生物传感器 · 分子诊断 · 转化医学 · 药物代谢
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JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY · 2019 · IF 4.027

Synthesis and biological evaluation of 3–(4-aminophenyl)-coumarin derivatives as potential anti-Alzheimer’s disease agents

Yu-Heng Hu,Jie Yang,Yun Zhang,Ke-Chun Liu,Teng Liu,Jie Sun,Xiao-Jing Wang

The work is focused on the design of drugs that prevent and treat Alzheimer’s disease (AD) and its complications. A series of 3–(4-aminophenyl)-coumarin derivatives designed, synthesised, fully characterised and evaluated in vitro/vivo. The biological assay experiments showed that some compounds displayed a clearly selective inhibition for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among all compounds, compound 4m exhibited the highest AChE inhibition with an IC50 value of 0.091 ± 0.011 µM and compound 4k exhibited the highest BuChE inhibition with an IC50 value of 0.559 ± 0.017 µM. A zebrafish behaviour analyser (Zebrobox) was used to determine the behavioural effects of the active compound on the movement distance of the aluminium chloride-induced zebrafish. Compound 4m offered a potential drug design concept for the development of therapeutic or preventive agents for AD and its complications.

研究领域: 药理学 · 神经科学 · 药物设计
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