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Terpenes and Phenylpropanoids as Acetyl- and Butyrylcholinesterase Inhibitors: A Comparative Study.
Current Alzheimer Research ( IF 1.8 ) Pub Date : 2019-01-01 , DOI: 10.2174/1567205016666191010105115
Dominik Szwajgier 1 , Ewa Baranowska-Wójcik 1
Affiliation  

BACKGROUND Cholinesterase inhibitors are routinely applied in the treatment of Alzheimer's disease, and seeking new cholinesterase inhibitors is a priority. OBJECTIVES Twenty seven compounds were compared, including ones not previously tested. An attempt was undertaken to precisely describe the role of alcohol in the inhibitory activity. This paper underlines the role of a "false positive" blank sample in the routine analysis. METHODS The inhibition of cholinesterase was measured using Ellman's colorimetric method with a few modifications designed by the authors (including the "false-positive" effect). The inhibitory role of ethanol and methanol was also carefully evaluated. The present and past results were compared taking the source of enzyme and alcohol content into consideration. RESULTS For the first time, new inhibitors were identified, namely: methyl jasmonate, 1R-(-)-nopol ((anti-acetyl-(AChE) and butyrylcholinesterase (BChE) activity)) and 1,4-cineole, allo-aromadendrene, nerolidol, β-ionone, and (R)-(+)-pulegone (anti-BChE activity). Oleanolic acid and (+)-β-citronellene (not previously studied) proved to be inefficient inhibitors. For a number of well-known inhibitors (such as nerol, (-)-menthol, (+)-menthol, isoborneol, (-)-bornyl acetate, limonene, α-pinene, β-pinene, α- ionone, and eugenol) some serious discrepancies were observed between our findings and the results of previous studies. Ethanol and methanol showed no anti-AChE activity up to 0.29% (v/v) and 0.23% (v/v), respectively. Similarly, ethanol up to 0.33% (v/v) and methanol up to 0.29% (v/v) did not inhibit the activity of BChE. CONCLUSION It can be stated that the impact of alcohol should be precisely determined and that blank "false-positive" samples should be processed together with test samples. Furthermore, the effect of the enzyme origin on the result of this test must be taken into consideration.

中文翻译:

萜烯和苯丙烷类化合物作为乙酰胆碱酯酶和丁酰胆碱酯酶的抑制剂:比较研究。

背景技术胆碱酯酶抑制剂常规地用于治疗阿尔茨海默氏病,并且寻找新的胆碱酯酶抑制剂是当务之急。目的比较了27种化合物,包括先前未测试过的化合物。试图精确描述醇在抑制活性中的作用。本文强调了“假阳性”空白样品在常规分析中的作用。方法采用Ellman比色法对胆碱酯酶的抑制作用进行了测定,作者对此进行了一些修改(包括“假阳性”效应)。还仔细评估了乙醇和甲醇的抑制作用。比较了目前和过去的结果,并考虑了酶和酒精含量的来源。结果第一次,确定了新的抑制剂,即:茉莉酸甲酯,1R-(-)-nopol((抗乙酰基-(AChE)和丁酰胆碱酯酶(BChE)活性))和1,4-桉树脑,别-芳香金属,神经节苷脂,β-紫酮和(R)-(+)-pulegone(抗BChE活性)。齐墩果酸和(+)-β-香茅烯(先前未研究)被证明是无效的抑制剂。对于许多众所周知的抑制剂(例如,神经醇,(-)-薄荷醇,(+)-薄荷醇,异冰片醇,(-)乙酸冰片酯,li烯,α-pine烯,β-pine烯,α-紫罗兰酮和丁香酚)在我们的发现和以前的研究结果之间发现了一些严重的差异。乙醇和甲醇分别显示高达0.29%(v / v)和0.23%(v / v)的抗AChE活性。类似地,高达0.33%(v / v)的乙醇和高达0.29%(v / v)的甲醇也不会抑制BChE的活性。结论可以说,应准确确定酒精的影响,空白“假阳性”样品应与测试样品一起处理。此外,必须考虑酶来源对该测试结果的影响。
更新日期:2019-11-01
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