目的 研究乌天麻Gastrodia elata二氯甲烷萃取部位的化学成分及其胆碱酯酶抑制活性。方法 采用Ellman法测定了二氯甲烷萃取部位对乙酰胆碱酯酶（acetyl cholinesterase，AChE）和丁酰胆碱酯酶（butyryl cholinesterase，BuChE）的抑制活性；利用硅胶柱色谱、Sephadex LH-20柱色谱、半制备高效液相色谱等方法进行分离纯化；利用NMR、MS等技术鉴定化合物结构；测定所有单体化合物的胆碱酯酶抑制活性。结果 乌天麻二氯甲烷萃取部位对AChE和BuChE均有显著的抑制活性，半数抑制浓度（median inhibition concentration，IC₅₀）分别为10.45、9.20μg/mL；从中分离得到11个化合物，分别鉴定为环[甘氨酸-l-S-(4''-羟基苯基)半胱氨酸]（1）、5'-甲硫基腺苷（2）、对羟基苄胺（3）、对羟基苯甲醇（4）、对羟基苯甲醛（5）、2-甲基-3-羟基吡啶（6）、4-乙酰氧甲苯基-β-D-吡喃葡萄糖苷（7）、4-(乙氧基甲基)苯酚β-D-吡喃葡萄糖苷（8）、小檗碱（9）、(＋)-thalirugidine（10）和(＋)-海兰地嗪（11）。结论 化合物1～3和9～11为首次从天麻属中分离得到。化合物9（IC₅₀＝5.93μmol/L）和10（IC₅₀＝42.49μmol/L）对AChE有抑制活性，化合物10（IC₅₀＝21.20μmol/L）对BuChE有抑制活性。

Objective To study the chemical constituents and cholinesterase inhibitory activity of the dichloromethane (CH₂Cl₂)-soluble fraction from Gastrodia elata f. glauca (Orchidaceae).Methods The Ellman method was used to determine the inhibitory activity of CH₂Cl₂-soluble fraction on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Silica gel column chromatography, Sephadex LH-20, semi-preparative HPLC and other methods were used for separation and purification. NMR and MS were used to identify the structures of the compounds. The cholinesterase inhibitory activity of all compounds was determined.Results The CH₂Cl₂-soluble fraction of G. elata f. glauca showed significant inhibitory activities on AChE (IC₅₀ = 10.45 μg/mL) and BuChE (IC₅₀ = 9.20 μg/mL). Eleven compounds were isolated from the CH₂Cl₂-soluble fraction by chromatography and identified as cyclo[glycine-l-S-(4''-hydroxybenzyl)cysteine] (1), 5'-S-methyl-5'-thioadenosine (2), 4-(aminomethyl)phenol (3), 4-(hydroxymethyl)phenol (4), 4-hydroxybenzaldehyde (5), 2-methylpyridin-3-ol (6), 4-[(acetyloxy)methyl] phenyl β-D-glucopyranoside (7), 4-(ethoxymethyl)phenol β-D-glucopyranoside (8), berberine (9), (＋)-thalirugidine (10) and (＋)-hernandezine (11) by spectroscopic methods.Conclusion Compounds 1-3 and 9-11 are isolated from G. elata f. glauca for the first time. Compounds 9 (IC₅₀ = 5.93 μmol/L) and 10 (IC₅₀ = 42.49 μmol/L) showed AChE-inhibitory activity, while 10 (IC₅₀ = 21.20 μmol/L) also showed inhibitory activity against BuChE.

R284.1

中国科学院科技扶贫项目(KFJ-FP-201905);云南省科技入滇项目(202003AD150005)