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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Presence of cholinomimetic and acetylcholinesterase inhibitory constituents in betel nut
Life Sciences, Volume 75, No. 20, Year 2004
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Description
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 μg/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 μg/mL) and physostigmine (0.1-3.0 μM) potentiated the effect of a fixed dose of ACh (10 μM) 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 μg/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. © 2004 Elsevier Inc. All rights reserved.
Authors & Co-Authors
Gilani, Anwar ul Hassan
Pakistan, Karachi
The Aga Khan University Medical College
Ghayur, Muhammad Nabeel
Pakistan, Karachi
The Aga Khan University Medical College
Pakistan, Karachi
University of Karachi
Saify, Zafar Saeed
Pakistan, Karachi
University of Karachi
Choudhary, Mohammed Iqbal
Pakistan, Karachi
University of Karachi
Khalid, Asaad
Pakistan, Karachi
University of Karachi
Statistics
Citations: 75
Authors: 5
Affiliations: 2
Identifiers
Doi:
10.1016/j.lfs.2004.03.035
ISSN:
00243205
Research Areas
Substance Abuse