微乳液对（L.）Willd.精油的胆碱酯酶抑制作用的增强。
Enhancement of Cholinesterase Inhibition of (L.) Willd. Essential Oil by Microemulsions.
机构信息
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand.
Research Center of Pharmaceutical Nanotechnology, Chiang Mai University, Chiang Mai 50200, Thailand.
出版信息
Molecules. 2022 May 19;27(10):3275. doi: 10.3390/molecules27103275.
This study aimed to investigate the chemical composition and reveal the selective inhibitory activity of (L.) Willd. essential oil (AGO) on acetylcholinesterase (AChE) compared to butyrylcholinesterase (BChE). The chemical composition of AGO was investigated by means of gas chromatography-mass spectrometry. Ellman's method was used to determine the inhibitory activities against AChE and BChE. Microemulsion systems with desirable anticholinesterase effects were developed. Methyl cinnamate and 1,8-cineole were reported as the major component of AGO. The IC values of oil against AChE and BChE were 24.6 ± 9.6 and 825.4 ± 340.1 µg/mL, respectively. The superior selectivity of AGO on AChE (34.8 ± 8.9) compared to galantamine hydrobromide (6.4 ± 1.5) suggested AGO to be an effective ingredient with fewer side effects for Alzheimer's treatment. Interestingly, the microemulsion of AGO possessed significantly higher anticholinesterase activity than that of native oil alone. Therefore, microemulsion of AGO is a promising alternative approach for the treatment of Alzheimer's disease.
本研究旨在调查（L.）Willd. 精油（AGO）的化学成分，并揭示其对乙酰胆碱酯酶（AChE）的选择性抑制活性，与丁酰胆碱酯酶（BChE）相比。通过气相色谱-质谱法研究了 AGO 的化学成分。采用 Ellman 法测定对 AChE 和 BChE 的抑制活性。开发了具有理想抗胆碱酯酶作用的微乳液体系。报告说，肉桂酸甲酯和 1,8-桉树脑是 AGO 的主要成分。油对 AChE 和 BChE 的 IC 值分别为 24.6 ± 9.6 和 825.4 ± 340.1 µg/mL。AGO 对 AChE 的选择性（34.8 ± 8.9）优于氢溴酸加兰他敏（6.4 ± 1.5），表明 AGO 是一种具有较少副作用的有效成分，可用于治疗阿尔茨海默病。有趣的是，AGO 的微乳液比单独的天然油具有更高的抗胆碱酯酶活性。因此，AGO 的微乳液是治疗阿尔茨海默病的一种很有前途的替代方法。
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