目的 研究瑞香科植物芫花Daphne genkwa干燥花蕾的化学成分及其对肿瘤细胞的抑制活性。方法 采用D101大孔吸附树脂、ODS反相硅胶、Sephadex LH-20凝胶、H/G正相硅胶以及半制备型高效液相等色谱柱色谱方法进行分离和纯化，并采用波谱数据和理化数据鉴定化合物的结构。同时采用CCK8法评估其抗肿瘤活性。结果 从芫花的乙醇提取物中分离得到15个化合物，分别鉴定为芹菜素（1）、3,7-二羟基-5,4'-二甲氧基黄酮（2）、3,5-二羟基-7,4'-二甲氧基黄酮（3）、木犀草素（4）、银椴苷（5）、西瑞香素（6）、胡萝卜苷（7）、金色酰胺醇酯（8）、橙黄胡椒酰胺乙酸酯/橙黄胡椒酰胺（9）、邻苯二甲酸二戊酯（10）、2-羟基-1-(3-羟基-3-(2-(2-甲氧基-2-氧乙基)苯基)丙酰氧基)戊烷-3-基苯甲酸酯（11）、3-(3,5-二叔丁基-4-羟基苯基)丙酸甲酯（12）、连翘脂素（13）、9-顺式-视黄醇棕榈酸酯（14）、正十九酸（15）。40.0 μmol/L时，化合物3对人肝癌HepG2细胞的生长有一定的抑制作用，其半数抑制浓度（median inhibition concentration，IC₅₀）值为（46.02±3.14）μmol/L；化合物2和12对BALB/c小鼠乳腺癌细胞4T1的生长有一定的抑制作用，其IC₅₀值分别为（53.11±1.73）、（54.67±0.99）μmol/L。各化合物对人宫颈癌HeLa-NH2细胞和小鼠单核巨噬细胞白血病RAW264.7细胞均没有明显毒性作用。结论 从芫花中分离得到15个化合物，其中化合物12为首次从芫花属植物中分离得到，化合物2、3、5、9、11、15为首次从芫花干燥花蕾中分离得到。化合物2、3和12具有潜在的抗肿瘤作用。

Objective To investigate the chemical constituents and anti-tumor activity of the dried buds of Daphne genkwa, a plant of the family Thymelaeaceae. Methods The structures of the compounds were separated and purified by column chromatography using D101, ODS, Sephadex LH-20, H/G silica gel and semi-preparative HPLC, and their structures were characterized by spectral data and physicochemical data. Effect on cell viability in four tumor cell models using the CCK-8 assay. Results A total of 15 compounds were obtained and identified as apigenin (1), 3,7-dihydroxy-5,4'-dimethoxyflavone (2), 3,5-dihydroxy-7,4'-dimethoxyflavone (3), luteolin (4), tiliroside (5), daphnoretin (6), daucosterol (7), aurantiamide acetate (8), aurantiamide (9), dipentyl phthalate (10), 2-hydroxy-1-(3-hydroxy-3-(2-(2-methoxy-2-oxoethyl)phenyl)propanoyloxy)pentan-3-ylbenzoate (11), methyl 3-(3,5-di-tert-butyl-4-hydroxyphenyl)propionate (12), phillygenin (13), 9-cis-retinyl palmitate (14), N-nonadecanoic acid (15). At a drug concentration of 40.0 μmol/L, compound 3 showed a certain inhibitory activity against the cell growth of HepG2, with an IC₅₀ value of (46.02 ±3.14) μmol/L. Compounds 2 and 12 showed moderate inhibitory activity against 4T1, with IC₅₀ values of (53. 11 ±1.73) μmol/L and (54.67 ±0.99) μmol/L, respectively, and there was no significant toxicity to HeLa-NH2 and RAW264.7. Conclusion 15 compounds were isolated from D. genkwa. Compound 12 was isolated from Daphne genus for the first time, while compounds 2, 3, 5, 9, 11 and 15 were isolated from the buds of D. genkwa for the first time. Compounds 2, 3 and 12 possessed potential anti-tumor effects.

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国家自然科学基金资助项目（31800293）；国家自然科学基金资助项目（32370422）；山西省自然科学基金资助项目（202203021211290，201901D211141）