Acetylcholinesterase immobilized capillary reactors coupled to protein coated magnetic beads: A new tool for plant extract ligand screening

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• 作者：Kenia Louren莽o Vanzolini ; Zhengjin Jiang ; Xiaoqi Zhang ; Lucas Campos Curcino Vieira ; Arlene Gon莽alvez Corr锚a ; Carmen Lucia Cardoso ; Quezia Bezerra Cass ; Ruin Moaddel
• 关键词：Binding affinities ; Acetylcholinesterase inhibitor ; Non-linear chromatography
• 刊名：Talanta
• 出版年：15 November, 2013
• 年：2013
• 卷：116
• 期：Complete
• 页码：647-652
• 全文大小：802 K

文摘

The use of immobilized capillary enzyme reactors (ICERs) and enzymes coated to magnetic beads ((NT or CT)-MB) for ligand screening has been adopted as a new technique of high throughput screening (HTS). In this work the selected target was the enzyme acetylcholinesterase (AChE), which acts on the central nervous system and is a validated target for the treatment of Alzheimer鈥檚 disease, as well as for new insecticides. A new approach for the screening of plant extracts was developed based on the ligand fishing experiments and zonal chromatography. For that, the magnetic beads were used for the ligand fishing experiments and capillary bioreactors for the activity assays. The latter was employed also under non-linear conditions to determine the affinity constants of known ligands, for the first time, as well as for the active fished ligand.