期刊
JOURNAL OF PHARMACY AND PHARMACOLOGY
卷 65, 期 12, 页码 1681-1700出版社
WILEY
DOI: 10.1111/jphp.12081
关键词
biomedicinal chemistry; clinical efficacy of natural products; drugs from natural sources; structure; activity relationships
资金
- Ciencia e a Tecnologia (FCT) [PEst-C/EQB/LA0006/2011]
- Consolider Ingenio [CSD2007-00063 FUN-C-FOOD]
- Grupo de Excelencia de la Region de Murcia [04486/GERM/06]
- FCT [SFRH/BD/63852/2009]
- CYTED Programme, Thematic Network Action [112RT0460]
- Fundação para a Ciência e a Tecnologia [SFRH/BD/63852/2009] Funding Source: FCT
ObjectivesAlzheimer's disease (AD) is the most common cause of dementia, being responsible for high healthcare costs and familial hardships. Despite the efforts of researchers, no treatment able to delay or stop AD progress exists. Currently, the available treatments are only symptomatic, cholinesterase inhibitors being the most widely used drugs. Here we describe several natural compounds with anticholinesterase (acetylcholinesterase and butyrylcholinesterase) activity and also some synthetic compounds whose structures are based on those of natural compounds. Key findingsGalantamine and rivastigmine are two cholinesterase inhibitors used in therapeutics: galantamine is a natural alkaloid that was extracted for the first time from Galanthus nivalisL., while rivastigmine is a synthetic alkaloid, the structure of which is modelled on that of natural physostigmine. Alkaloids include a high number of compounds with anticholinesterases activity at the submicromolar range. Quinones and stilbenes are less well studied regarding cholinesterase inhibition, although some of them, such as sargaquinoic acid or (+)--viniferin, show promising activity. Among flavonoids, flavones and isoflavones are the most potent compounds. Xanthones and monoterpenes are generally weak cholinesterase inhibitors. SummaryNature is an almost endless source of bioactive compounds. Several natural compounds have anticholinesterase activity and others can be used as leader compounds for the synthesis of new drugs.
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