目的 研究中药白及的化学成分及其抗肿瘤活性,并对其抗肿瘤活性的作用机制做细胞周期的探讨。方法 采用正、反相硅胶柱、凝胶柱,通过波谱分析进行结构鉴定;采用MTT方法进行化合物的抗肿瘤活性筛选,采用流式细胞仪检测化合物对细胞周期的影响。结果 从中药白及中分离得到5个化合物,经波谱数据分析分别鉴定为齐墩果酸-3-O-α-L-鼠李糖-(1→2)-β-D-吡喃葡萄糖苷(1),2-羟基丁二酸(2),对羟基苄胺(3),棕榈酸(4)和对羟基苯甲酸(5)。化合物1具抗肿瘤活性,且其能够诱导A549细胞周期阻滞于G₀/G₁期。结论 化合物1~4均为首次从白及中分离得到,其中化合物1具有一定的抗肿瘤活性,其作用机制与细胞周期阻滞相关。

OBJECTIVE To investigate the chemical constituents from Bletilla striata (Thunb.) Reichb.f and study their anti-tumor activities and effect on progression of cell cycle. METHODS The compounds were isolated by various chromatographic methods including silica gel, ODS, Sephadex LH-20, and so on. Their structures were identified by extensive analysis of spectiroscopic data. The antiproliferative effects of the compounds were evaluated using MTT test, and compound 1 was tested for the effect on the cell cycle of A549 cells. RESULTS Five compounds were isolated from Bletilla striata and identified as 3β-hydroxyoleane-12-en-28-oic acid 3-O-α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranoside(1),2-hydroxysuccinic acid(2),4-hydroxybenzylamine(3),palmitic acid(4),and 4-hydroxybenzoic acid(5). Compound 1 showed antiproliferative activity against the cancer cells and could induce G₀/G₁ phase arrest effectively after 24 h treatment. CONCLUSION Compounds 1-4 are isolated from Bletilla striata for the first time. Compound 1 shows potent inhibitory effect and might produce their action through inducing cell cycle arrest.