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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
20
pubmed:dateCreated
2004-9-7
pubmed:abstractText
In this investigation, we report the presence of cholinomimetic and acetylcholinesterase (AChE) inhibitory constituents in betel nut, the most commonly used drug in the world after tobacco, ethanol and caffeine. The crude extract of betel nuts or Areca catechu (Ac.Cr) caused a dose-dependent (0.3-300 microg/mL) spasmogenic effect in the isolated rabbit jejunum. The spasmogenic effect was blocked by atropine, similar to that of acetylcholine (ACh), suggestive of muscarinic receptor mediated effect. Both the extract (0.3-10 microg/mL) and physostigmine (0.1-3.0 microM) potentiated the effect of a fixed dose of ACh (10 microM) in a dose-dependent fashion, suggesting acetylcholinesterase (AChE) inhibitory effect. This effect was confirmed in the in vitro assay where both the crude extract (1-100 microg/mL) and physostigmine inhibited the enzyme. In the in vivo model of gastrointestinal transit, Ac.Cr (10-30 mg/kg) enhanced the travel of charcoal meal and also exhibited a laxative effect in mice. The plant extract was subjected to activity-directed fractionation and all resultant fractions showed atropine-sensitive spasmogenicity in rabbit jejunum and also AChE inhibitory effect at doses similar to that for the parent crude extract, the ethyl acetate fraction being slightly less potent. Some of the known constituents of betel nut, including arecoline, were tested for the possible inhibitory effect on AChE, none were found active. The study provides first evidence for the presence of AChE inhibitory constituents in betel nut, though additional direct muscarinic stimulatory effect cannot be ruled out and this study provides sound scientific basis for some of the folkloric uses associated with betel nut chewing.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0024-3205
pubmed:author
pubmed:issnType
Print
pubmed:day
1
pubmed:volume
75
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2377-89
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed-meshheading:15350815-Acetylcholine, pubmed-meshheading:15350815-Acetylcholinesterase, pubmed-meshheading:15350815-Animals, pubmed-meshheading:15350815-Areca, pubmed-meshheading:15350815-Atropine, pubmed-meshheading:15350815-Cholinergic Agonists, pubmed-meshheading:15350815-Cholinesterase Inhibitors, pubmed-meshheading:15350815-Dose-Response Relationship, Drug, pubmed-meshheading:15350815-Female, pubmed-meshheading:15350815-Jejunum, pubmed-meshheading:15350815-Male, pubmed-meshheading:15350815-Mice, pubmed-meshheading:15350815-Mice, Inbred BALB C, pubmed-meshheading:15350815-Muscarinic Antagonists, pubmed-meshheading:15350815-Physostigmine, pubmed-meshheading:15350815-Plant Extracts, pubmed-meshheading:15350815-Rabbits, pubmed-meshheading:15350815-Receptors, Muscarinic, pubmed-meshheading:15350815-Vasodilator Agents
pubmed:year
2004
pubmed:articleTitle
Presence of cholinomimetic and acetylcholinesterase inhibitory constituents in betel nut.
pubmed:affiliation
Department of Biological and Biomedical Sciences, The Aga Khan University Medical College, Karachi-74800, Pakistan. anwar.gilani@aku.edu
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't