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目的:研究蓝花黄芩的黄酮成分及其抗肿瘤活性。方法:采用硅胶柱层析、制备薄层色谱法、Sephadex LH-20柱色谱和重结晶等方法进行分离纯化,根据理化性质和波谱数据鉴定化合物结构,采用MTT法测定了化合物对Hela、MCF7和A549人肿瘤细胞株的细胞毒活性。结果:从蓝花黄芩中分离鉴定了10个黄酮类化合物,分别为:5,7-二羟基-8,2’-二甲氧基黄酮(1)、5-羟基-7,8,2’,6’-四甲氧基黄酮(2)、5,7-二羟基-6-甲氧基黄酮(3)、5,7-二羟基-8-甲氧基黄酮(4)、5,7,4’-三羟基-8-甲氧基黄酮(5)、5,7,2’-三羟基-8-甲氧基黄酮(6)、5-羟基-7,8,2’,6’-四甲氧基二氢黄酮(7)、5,7-二羟基-8,2’-二甲氧基二氢黄酮(8)、5,7,2’-三羟基-8-甲氧基二氢黄酮(9)、5,7-二羟基二氢黄酮(10)。化合物6对Hela、MCF-7和A549细胞的IC_(50)值分别为35.7、37.0、35.6μg/m L,化合物7对Hela和MCF-7细胞的IC50值分别为35.0、37.8μg/m L。结论:从蓝花黄芩中共分得10个黄酮类化合物,所有化合物均为首次从该植物中分离得到。化合物6和7显示微弱的肿瘤细胞毒活性。
Objective: To study the flavonoids of Scutellaria baicalensis and its anti-tumor activity. Methods: The compounds were separated and purified by silica gel column chromatography, preparative thin layer chromatography, Sephadex LH-20 column chromatography and recrystallization. The structures of compounds were identified by their physico-chemical properties and spectral data. The compounds were determined by MTT assay. Cytotoxic activity of A549 human tumor cell line. Results: Ten flavonoids were isolated from Scutellaria baicalensis and identified as 5,7-dihydroxy-8,2’-dimethoxyflavone (1), 5-hydroxy-7,8,2 ’ (2), 5,7-dihydroxy-6-methoxyflavone (3), 5,7-dihydroxy-8-methoxyflavone (4), 5,7 Trihydroxy-8-methoxyflavone (5), 5,7,2’-trihydroxy-8-methoxyflavone (6), 5- hydroxy-7,8,2 ’, 6’ Tetramethoxyflavone (7), 5,7-dihydroxy-8,2’-dimethoxyflavanone (8), 5,7,2’-trihydroxy-8-methoxy Flavanone (9), 5,7-dihydroxyflavone (10). IC50 values of compound 6 in Hela, MCF-7 and A549 cells were 35.7, 37.0 and 35.6 μg / ml, respectively. IC50 values of compound 7 in Hela and MCF-7 cells were 35.0 and 37.8 μg / ml, respectively . CONCLUSION: Ten flavonoids were isolated from Scutellaria baicalensis Georgi, and all the compounds were isolated from this plant for the first time. Compounds 6 and 7 show weak tumor cytotoxic activity.