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综合运用硅胶、MCI、Sephadex LH-20等柱色谱及高效液相色谱技术对小蓟的乙酸乙酯部位进行分离纯化,从中分离得到黄酮类化合物15个,分别鉴定为:4’,5,6-三羟基-7-甲氧基黄酮(1),4’,5-二羟基-7,8-二甲氧基黄酮(2),sorbifolin-6-O-β-glucopyranoside(3),山柰酚-7-O-α-L-鼠李糖苷(4),山柰酚(5),槲皮素-3-O-β-D-葡萄糖-7-O-α-L-鼠李糖苷(6),myricetin(7),myricetin-3-O-β-D-glucoside(8),5,7-二羟基-3’,4’-二甲氧基黄酮(9),3’,4’,5-三羟基-3,7-二甲氧基黄酮(10),3’,3,4’,5-四羟基-7-甲氧基黄酮(11),3’-羟基-4’,5,7-三甲氧基黄酮(12),7-羟基-3’,4’,5-三甲氧基黄酮(13),4’,5-二羟基-2’,3’,7,8-四甲氧基黄酮(14),5-羟基-2’,3’,7,8-四甲氧基黄酮(15)。以上所有化合物均为首次从本植物中分离得到。该实验运用PTP1B抑制剂高通量筛选模型对化合物(1~15)进行活性筛选,结果表明化合物2,12和14具有较强的PTP1B抑制活性,IC50分别为2.54,1.85,2.11μmol·L~(-1)。
The ethyl acetate fraction of Artemisia annuus was isolated and purified by silica gel, MCI, Sephadex LH-20 column chromatography and high performance liquid chromatography (HPLC). Fifteen flavonoid compounds were isolated and identified as 4 ’, 5,6 - trihydroxy-7-methoxyflavone (1), 4 ’, 5-dihydroxy-7,8-dimethoxyflavone (2), sorbifolin- 6-O-β-glucopyranoside 7-O-α-L-rhamnoside (4), kaempferol (5), quercetin-3-O-β-D-glucose-7- Myricetin (7), myricetin-3-O-β-D-glucoside (8), 5,7-dihydroxy-3 ’, 4’-dimethoxyflavone (9), 3’, 4 ’ (10), 3 ’, 3,4’, 5-tetrahydroxy-7-methoxyflavone (11), 3’-hydroxy-4 ’ Trimethoxyflavone (12), 7-hydroxy-3 ’, 4’, 5-trimethoxyflavone (13), 4 ’, 5-dihydroxy-2’, 3 ’, 7,8- Tetramethoxyflavone (14), 5-hydroxy-2 ’, 3’, 7,8-tetramethoxyflavone (15). All of the above compounds are isolated from this plant for the first time. In this experiment, the compounds (1-15) were screened by high-throughput screening of PTP1B inhibitors. The results showed that compounds 2, 12 and 14 had strong PTP1B inhibitory activity with IC50 of 2.54, 1.85 and 2.11 μmol·L- (-1).