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目的研究海蒿子Sargassum pallidum的化学成分及其体外抗肿瘤活性。方法采用硅胶柱色谱法、凝胶色谱法和制备液相色谱法分离化合物,运用波谱技术鉴定化合物的结构,并利用流式细胞术评价化合物的抗肿瘤活性。结果从海蒿子70%乙醇提取物中分离得到了11个化合物,分别鉴定为aurantiamide(Ⅰ)、benzoylphe-nylalaninol(Ⅱ)、胸腺嘧啶脱氧核苷(Ⅲ)、邻苯二甲酸异丁酯(Ⅳ)、2′,5-二羟基-6,6′,7,8-四甲氧基黄酮(Ⅴ)、5,6-二羟基-7-甲氧基黄酮(Ⅵ)、5,7-二羟基-8-甲氧基黄酮(Ⅶ)、4-hydroxyphthalide(Ⅷ)、2-amino-3-phenylpropyl acetate(Ⅸ)、4(1H)-quinolinone(X)和2-benzothiazolol(Ⅺ)。其中化合物Ⅲ对tsFT210细胞有较强的坏死性细胞毒活性,其IC_(50)为0.50μmol/L;化合物Ⅴ、X对K562细胞,以及化合物Ⅴ、Ⅷ对P388细胞,显示细胞周期(G_0/G_1期)抑制活性。结论化合物Ⅰ～Ⅺ均为首次从海蒿子中分离得到。
Objective To study the chemical constituents of Sargassum pallidum and its anti-tumor activity in vitro. Methods The compounds were isolated by silica gel column chromatography, gel chromatography and preparative liquid chromatography. The structures of compounds were identified by spectroscopic techniques. The antitumor activity of the compounds was evaluated by flow cytometry. Results Eleven compounds were isolated from 70% ethanol extract of Artemisia annua and identified as aurantiamide (Ⅰ), benzoylphe-nylalaninol (Ⅱ), thymidine (Ⅲ) and isobutyl phthalate ), 2 ’, 5-dihydroxy-6,6’, 7,8-tetramethoxyflavone (V), 5,6-dihydroxy-7-methoxyflavone Hydroxy-8-methoxyflavone (VII), 4-hydroxyphthalide (VIII), 2-amino-3-phenylpropyl acetate (IX), 4 (1H) -quinolinone (X) and 2-benzothiazolol (XI). Among them, compound ¢ ó and ¢ ò had a strong necrotic cytotoxic activity against tsFT210 cells with an IC50 of 0.50|Ìmol / L. Compounds ¢ ô and X showed significant differences in cell cycle (G0 / G_1 phase) inhibitory activity. Conclusions Compounds Ⅰ ~ XI were isolated from sea cucumber for the first time.