目的 研究华泽兰Eupatorium chinense根部的化学成分及其药理活性。方法 采用正相硅胶柱色谱、薄层硅胶色谱、凝胶柱色谱及半制备高效液相色谱等色谱方法进行分离纯化，并通过现代波谱技术鉴定化合物结构。对化合物开展体外药理活性研究，选取α-葡萄糖苷酶和乙酰胆碱酯酶作为体外活性研究靶点，并利用分子对接技术计算化合物分别与α-葡萄糖苷酶和乙酰胆碱酯酶的相互作用。结果 从华泽兰根部分离得到6个单体化合物，分别鉴定为 (2S,3R)-2-((R)-1,2-二羟丙-2-基)-3-羟基-2,3-二氢苯并呋喃-5-基乙酮（1）、(2R,3S)-3-羟基-2-(2-羟基-2-丙基)-7-甲氧基-2,3-二氢苯并呋喃-5-基乙酮（2）、12,13-二羟基泽兰素（3）、泽兰酮（4）、泽兰素（5）、(2S,3R)-7-hydroxytoxol（6）。体外药理活性实验表明，化合物2、5、6对α-葡萄糖苷酶的半数抑制浓度（median inhibition concentration，IC₅₀）值分别为0.15、10.33、1.30 μg/mL；化合物1、3～5对乙酰胆碱酯酶的IC₅₀值分别为139.35、104.66、63.60、0.75 μg/mL。分子对接分析结果显示，化合物2、5和6与α-葡萄糖苷酶的对接结合能分别为−8.1、−7.7、−7.8 kcal/mol；化合物1、3、4和5与乙酰胆碱酯酶的对接结合能分别为−6.1、−6.7、−8.9、−5.9 kcal/mol。结论 化合物1和2为新化合物。分别命名为泽兰苯并呋喃F（1）和泽兰苯并呋喃H（2）。化合物6首次从华泽兰植物中分离得到。化合物2、5和6对α-葡萄糖苷酶呈现良好的抑制活性（IC₅₀＜20 μg/mL）；化合物1、3～5对乙酰胆碱酯酶表现出良好的抑制活性（IC₅₀＜200 μg/mL）。化合物2、5和6与α-葡萄糖苷酶蛋白结合能结合情况较好；化合物1、3～5与乙酰胆碱酯酶蛋白结合能结合作用较强。

Objective To investigate the chemical constituents of Eupatorium chinense roots and their pharmacological activities. Methods Compounds were purified and separated by using chromatographic methods such as normal-phase silica gel column chromatography, thin-layer silica gel chromatography, gel column chromatography and semi-preparative high performance liquid. The isolated compounds were evaluated for in vitro inhibitory potential against α-glucosidase and acetylcholinesterase, and molecular docking was employed to calculate their respective binding interactions with above two enzymes. Results A total of six monomeric compounds were isolated and identified as (2S,3R)-2-((R)-1,2-dihydroxypropan-2-yl)-3-hydroxy-2,3-dihydrobenzofuran-5-yl ethenone (1), (2R,3S)-3-hydroxy-2-(2-hydroxypropan-2-yl)-7-methoxy-2,3-dihydrobenzofuran-5-yl ethenone (2), 12,13-dihydroxyeuparin (3), euparone (4), euparin (5), and (2S,3R)-7-hydroxytoxol (6). In vitro pharmacological activity experiments showed that compounds 2, 5 and 6 exhibited potent inhibitory activity against α-glucosidase with median inhibition concentration (IC₅₀) values of 0.15, 10.33 and 1.30 μg/mL, respectively. Compounds 1, 3, 4 and 5 displayed notable acetylcholinesterase inhibitory effects with IC₅₀ values of 139.35, 104.66, 63.60 and 0.75 μg/mL, respectively. Molecular docking analyses revealed that compounds 2, 5, and 6 exhibited docking scores of −8.1, −7.7, and −7.8 kcal/mol, respectively, toward α-glucosidase, whereas compounds 1, 3, 4, and 5 displayed scores of −6.1, −6.7, −8.9, and −5.9 kcal/mol, respectively, against acetylcholinesterase. Conclusion Compounds 1 and 2 were new compounds, and named eupbenzofuran F (1) and eupbenzofuran H (2), respectively. Compound 6 was isolated from E. chinense for the first time. Compounds 2, 5 and 6 represented good inhibitory activity against α-glucosidase (IC₅₀< 20 μg/mL), whereas 1, 3, 4 and 5 may exhibit good inhibitory activity against acetylcholinesterase (IC₅₀< 200 μg/mL). Compounds 2, 5, and 6 showed favorable binding affinities to α-glucosidase, whereas compounds 1, 3, 4, and 5 exhibited strong interactions with acetylcholinesterase.

R284.1

国家自然科学基金资助项目（81803383）；湖北省科技创新基地（平台）计划（2025CSA044）；湖北省中央引导地方科技发展资金项目（2024BSB016）；三峡大学2025年度大学生创新创业训练计划项目（NO.174、179、292）；天然产物研究与利用湖北省重点实验室开放课题（2025NPRD06，2025NPRD07）