目的 对尖尾芋Alocasia cucullata的根茎进行化学成分及其抗肿瘤活性研究。方法 采用80%乙醇加热回流提取，依次用二氯甲烷、醋酸乙酯、正丁醇萃取，用AB-8大孔吸附树脂、正相硅胶柱、ODS硅胶柱、Sephadex LH-20凝胶柱和制备型液相色谱对提取物进行分离纯化。根据化合物的波谱数据和理化性质进行结构鉴定。同时采用CCK-8检测法，以星形孢菌素（staurosporine，STSP）作为阳性对照，对化合物进行体外抗肿瘤活性实验。结果 从尖尾芋根茎的80%乙醇提取物中分离鉴定出17个化合物，包括7个生物碱类、3个长链脂肪酸类、4个萜类、3个甾体类，分别鉴定为3-吲哚甲醛（1）、黄胡椒酰胺（2）、5-羟基-1H-吲哚-3-甲醛（3）、(3R,8aS)-六氢-3-(2-甲基丙基)吡咯并[1,2-a]吡嗪-1,4-二酮（4）、新刺孢曲霉素A（5）、N-顺式-阿魏酰酪胺（6）、N-反式-阿魏酰酪胺（7）、(–)-β-谷甾醇（8）、(22E)-麦角甾-6,9,22-三烯-3β,5β,8α-三醇（9）、(22E)-麦角甾-6,22-二烯-3β,5β,8α-三醇（10）、(S)-5-羟基-3,4-二甲基-5-戊基呋喃-2(5H)-酮（11）、地芰普内酯（12）、表-地芰普内酯（13）、蚱蜢酮（14）、苯十三烷酸（15）、(16Z)-16-十八烯-12,14-二炔酸（16）、(13S)-羟基-十八碳二烯酸（17）。化合物9和10对人乳腺癌MCF-7细胞半数抑制浓度（median inhibition concentration，IC₅₀）值分别为32.13、31.49 μmol/L。结论 化合物1～3、9～17为海芋属首次分离，化合物4、5是尖尾芋首次分离得到。抗肿瘤活性实验结果表明，化合物9和10对MCF-7细胞具有增殖抑制作用。

Objective To elucidate the bioactive substances in Alocasia cucullata and test their antitumor activities. Methods A 80% ethanol extract of A. cucullate was partitioned with dichloromethane (DCM), ethyl acetate (EtOAc), and n-butanol. The extracts were separated and purified by AB-8 macroporous adsorbent resin, positive phase silica gel column, ODS silica gel column, Sephadex LH-20 gel column, and preparative liquid chromatography. Their structures were identified by spectroscopic data and physiochemical properties. The compounds were subjected to evaluation of antitumor activities in vitro using CCK-8 assay with staurosporine (STSP) as the positive control. Results A total of 17 compounds, including seven alkaloids, three long-chain fatty acids, four terpenoids, and three steroids were isolated from the 80% ethanol extract of A. cucullate, and the structures were identified as indole-3-carboxaldehyde (1), aurantiamide (2), 5-hydroxy-1H-indole-3-carboxaldehyde (3), (3R,8aS)-hexahydro-3-(2-methylpropyl) pyrrolo[1,2-a]pyrazine-1,4-dione (4), neoechinulin A (5), N-cis-feruloyl tyramine (6), N-trans-feruloyl tyramine (7), (-)-β-sitosterol (8), (22E)-ergosta-6,9,22-triene-3β,5β,8α-triol (9), (22E)-ergosta-6,22-diene-3β,5β,8α-triol (10), (S)-5-hydroxy-3,4-dimethyl-5-pentylfuran-2(5H)-one (11), loliolide (12), (＋)-epi-loliolide (13), grasshopper ketone (14)，benzenetridecanoic acid (15), (16Z)-16-octadecene-12,14-diynoic acid (16), and (13S)-hydroxyoctadecadienoic acid (17). Compounds 9 and 10 exhibited the inhibitory effects on human breast cancer MCF-7 cells with median inhibition concentration (IC₅₀) values of 32.13, 31.49 μmol·L^-1, respectively. Conclusion Compounds 1—3 and 9—17 were isolated for the first time from the genus Alocasia, and compounds 4 and 5 were isolated for the first time from this plant. The results of antitumor activity showed that compounds 9 and 10 had proliferation inhibition against human breast cancer MCF-7 cells.

R284.1

广东省中医药局科研项目（20221290）;广东省医学科研基金项目（A2023416）