期刊
MOLECULES
卷 19, 期 7, 页码 8933-8948出版社
MDPI
DOI: 10.3390/molecules19078933
关键词
Alzheimer's disease; muscarinic acetylcholine receptor; binding activity; flavonoids; molecular modelling
资金
- Ministry of Education, Malaysia [ER002-2012A]
- University of Malaya [FS143/2007C, PS201/2010B]
- Victorian Life Sciences Computational Infrastructure [VR0133]
Muscarinic acetylcholine receptor-active compounds have potential for the treatment of Alzheimer's disease. In this study, a series of natural and synthetic flavones and flavonols was assayed in vitro for their ability to inhibit radioligand binding at human cloned M-1 muscarinic receptors. Several compounds were found to possess competitive binding affinity (K-i = 40-110 mu M), comparable to that of acetylcholine (K-i = 59 mu M). Despite the fact that these compounds lack a positively-charged ammonium group under physiological conditions, molecular modelling studies suggested that they bind to the orthosteric site of the receptor, mainly through non-polar interactions.
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