标准大麻素富组分乙酰胆碱酯酶抑制活性研究

Wiwit Suttithumsatid, Jiraporn Kara, Luelak Lomlim, Charassri Nualsri
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摘要

背景:由于大麻在许多国家被合法允许用于医疗目的,它已成为最令人感兴趣的问题,特别是在阿尔茨海默病(AD)等神经系统疾病方面。抑制乙酰胆碱酯酶(AChE)是治疗AD的机制之一。目的:建立富大麻素提取物的制备方法,并测定其乙酰胆碱酯酶抑制活性。方法:采用微波辅助提取(MAE) -疏水柱分离绿色提取工艺制备富含大麻素的提取物。采用高效液相色谱法测定大麻二酚(CBD)和Δ-9-tetrahydrocannabinol (THC)的含量。以电鳗乙酰胆碱酯为原料,采用光度法测定其体外抑酶活性。结果:不同浓度CBD和四氢大麻酚得到3个富含大麻素的组分,即ⅰ组分(CBD为8.1% w/w;THC为52.2% w/w), II (CBD为9.2% w/w;THC为8.0% w/w), III (CBD 1.3% w/w, THC 33.5% w/w)。这些富含大麻素的提取物具有AChE抑制活性,IC50值分别为52.3、59.8和71.2µg/mL。结论:该发现提示CBD可能是抑制乙酰胆碱酯酶的活性化合物,而非四氢大麻酚。
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Acetylcholinesterase Inhibitory Activity of Standardized Cannabinoids-rich Fractions
Background: Since cannabis has been legally allowed for medicinal purposes in many countries, it has become the most interesting issue, particularly in neurologic disorders, such as Alzheimer’s disease (AD). Inhibition of acetylcholinesterase (AChE) is one of the mechanisms for the treatment of AD. Objectives: The present study aimed to establish a method for the preparation of cannabinoid-rich extracts and determine their AChE inhibitory activity. Methods: The cannabinoid-rich extracts were prepared through a green extraction process using microwave-assisted extraction (MAE) followed by hydrophobic column separation. The contents of cannabidiol (CBD) and Δ-9-tetrahydrocannabinol (THC) were determined using high-performance liquid chromatography (HPLC). In vitro AChE inhibitory activity was determined via the photometric method using AChE from Electrophorus electricus. Results: Three cannabinoids-rich fractions were obtained with different concentrations of CBD and THC, namely Fractions I (CBD of 8.1% w/w; THC of 52.2% w/w), II (CBD of 9.2% w/w; THC of 8.0% w/w), and III (CBD 1.3% w/w, THC 33.5% w/w). These cannabinoid-rich extracts exhibited AChE inhibitory activity, with IC50 values of 52.3, 59.8, and 71.2 µg/mL, respectively. Conclusion: This finding suggests that CBD, but not THC, might be an active compound contributing to AChE inhibitory effect.
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