目的 研究瑞香科植物芫花Daphne genkwa干燥花蕾的化學(xué)成分及其對腫瘤細(xì)胞的抑制活性。方法 采用D101大孔吸附樹脂、ODS反相硅膠、Sephadex LH-20凝膠、H/G正相硅膠以及半制備型高效液相等色譜柱色譜方法進(jìn)行分離和純化，并采用波譜數(shù)據(jù)和理化數(shù)據(jù)鑒定化合物的結(jié)構(gòu)。同時(shí)采用CCK8法評估其抗腫瘤活性。結(jié)果 從芫花的乙醇提取物中分離得到15個(gè)化合物，分別鑒定為芹菜素（1）、3,7-二羥基-5,4'-二甲氧基黃酮（2）、3,5-二羥基-7,4'-二甲氧基黃酮（3）、木犀草素（4）、銀椴苷（5）、西瑞香素（6）、胡蘿卜苷（7）、金色酰胺醇酯（8）、橙黃胡椒酰胺乙酸酯/橙黃胡椒酰胺（9）、鄰苯二甲酸二戊酯（10）、2-羥基-1-(3-羥基-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-羥基苯基)丙酸甲酯（12）、連翹脂素（13）、9-順式-視黃醇棕櫚酸酯（14）、正十九酸（15）。40.0 μmol/L時(shí)，化合物3對人肝癌HepG2細(xì)胞的生長有一定的抑制作用，其半數(shù)抑制濃度（median inhibition concentration，IC₅₀）值為（46.02±3.14）μmol/L；化合物2和12對BALB/c小鼠乳腺癌細(xì)胞4T1的生長有一定的抑制作用，其IC₅₀值分別為（53.11±1.73）、（54.67±0.99）μmol/L。各化合物對人宮頸癌HeLa-NH2細(xì)胞和小鼠單核巨噬細(xì)胞白血病RAW264.7細(xì)胞均沒有明顯毒性作用。結(jié)論 從芫花中分離得到15個(gè)化合物，其中化合物12為首次從芫花屬植物中分離得到，化合物2、3、5、9、11、15為首次從芫花干燥花蕾中分離得到。化合物2、3和12具有潛在的抗腫瘤作用。

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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國家自然科學(xué)基金資助項(xiàng)目（31800293）；國家自然科學(xué)基金資助項(xiàng)目（32370422）；山西省自然科學(xué)基金資助項(xiàng)目（202203021211290，201901D211141）