小蓟中黄酮类化学成分的研究

Studies on flavonoids from Cirsium setosum

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)。

To investigate the chemical constituents of ethyl acetate from Cirsium setosum,fifteen flavonoids were obtained by column chromatography on silica gel,MCI,Sephadex LH-20,and preparative HPLC. Their structures were identified as 4＇,5,6-trihydroxy-7-methoxyflavone（ 1）,4＇,5-dihydroxy-7,8-dimethoxyflavone（ 2）,sorbifolin-6-O-β-glucopyranoside（ 3）,kaempferol-7-O-α-L-rhamnoside（ 4）,kaempferol（ 5）,quercetin-3-O-β-D-glucosyl-7-O-α-L-rhamnoside（ 6）,myricetin（ 7）,myricetin-3-O-β-D-glucoside（ 8）,5,7-dihydroxy-3＇,4＇-dimethoxyflavone（ 9）,3＇,4＇,5-trihydroxy-3,7-dimethoxyflavone（ 10）,3＇,3,4＇,5-tetrahydroxy-7-methoxyflavone（ 11）,3＇-hydroxy-4＇,5,7-trimethoxyflavone（ 12）,7-hydroxy-3＇,4＇,5-trimethoxyflavone（ 13）,4＇,5-dihydroxy-2＇,3＇,7,8-tetramethoxylflavone（ 14）,and 5-hydroxy-2＇,3＇,7,8-tetramethoxylflavone（ 15） by spectroscopic data analysis. All compounds were isolated from this plant for the first time. Compounds（ 1-15） were evaluated for their hypoglycemic activities by PTP1 B enzyme model. Among them,compounds 2,12,and 14 showed significant PTP1 B inhibitory activities with IC50 values of 2. 54,1. 85,2. 11 μmol · L^（-1）,respectively.