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Presence of cholinomimetic and acetylcholinesterase inhibitory constituents in betel nut

机译：槟榔中存在拟胆碱和乙酰胆碱酯酶抑制成分

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摘要

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 mug/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 mug/mL) and physostigmine (0.1-3.0 muM) potentiated the effect of a fixed dose of ACh (10 muM) 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 mug/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. (C) 2004 Elsevier Inc, All rights reserved.
机译：在这项调查中，我们报告了槟榔中存在拟胆碱和乙酰胆碱酯酶（AChE）抑制成分，槟榔是继烟草，乙醇和咖啡因之后世界上最常用的药物。槟榔或槟榔（Ac.Cr）的粗提物对离体的兔空肠产生剂量依赖性（0.3-300 cup / mL）的痉挛作用。阿托品阻断了痉挛作用，类似于乙酰胆碱（ACh），暗示了毒蕈碱受体介导的作用。提取物（0.3-10杯/毫升）和毒扁豆碱（0.1-3.0微米）均以剂量依赖的方式增强了固定剂量的乙酰胆碱酯（10微米）的作用，表明乙酰胆碱酯酶（AChE）具有抑制作用。这种作用在体外测定中得到了证实，粗提取物（1-100杯/毫升）和毒扁豆碱均抑制了该酶。在胃肠道运输的体内模型中，Ac.Cr（10-30 mg / kg）增强了木炭粉的行程，并且在小鼠中也表现出通便的作用。将植物提取物进行活性导向的分级分离，并且所有得到的级分在兔空肠中均显示出对阿托品敏感的痉挛性，并且在与母体粗提取物相似的剂量下也显示出对AChE的抑制作用，乙酸乙酯级分的效力略低。测试了槟榔的一些已知成分（包括槟榔碱）对AChE的可能抑制作用，但均未发现有活性。该研究为槟榔中存在AChE抑制成分提供了第一个证据，尽管不能排除其他直接的毒蕈碱刺激作用，并且该研究为与槟榔咀嚼相关的某些民俗用途提供了可靠的科学依据。 （C）2004 Elsevier Inc，保留所有权利。

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