Nature as a source of metabolites with cholinesterase-inhibitory activity: an approach to Alzheimer's disease treatment

• Type: Another Publication in an International Scientific Journal
• Date: 2013

Authors

Brigida R Pinho (Author) Other; Federico Ferreres (Author) Other; Patricia Valentao (Author) FFUP; Paula B Andrade (Author) FFUP

Journal

Title: Journal of Pharmacy and Pharmacology

Vol. 65

Pages: 1681-1700

ISSN: 0022-3573

Publisher: Oxford University Press

Indexing

ISI Web of Knowledge - 46 Citations

Scopus - 64 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-008-H12

DOI: 10.1111/jphp.12081

Abstract (EN): 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.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 20