板蓝根抗病毒有效部位的化学成分及其活性研究

Chemical constituents in antiviral fraction of Isatidis Radix and their activities

目的研究板蓝根Isatidis Radix抗病毒有效部位的化学成分及单体成分的活性。方法板蓝根水提物经D101大孔树脂吸附,10%、50%乙醇洗脱的有效部位,经硅胶柱色谱、反相硅胶柱色谱及Sephadex LH-20进行分离纯化,并根据理化常数和波谱数据,鉴定化合物的结构。结果从板蓝根水提抗病毒有效部位中分离得到10个化合物,分别鉴定为丁香苷(1)、4-(1,2,3-三羟基丙基)-2,6-二甲氧基苯-1-O-β-D-葡萄糖苷(2)、异落叶松脂醇(3)、异落叶松脂醇-4-O-β-D-葡萄糖苷(4)、落叶松脂素-4-O-β-D-葡萄糖苷(5)、落叶松脂素-4,4′-二-O-β-D-二葡萄糖苷(6)、2-羟基-1,4-苯二甲酸(7)、D-甘露醇(8)、吲哚-3-乙腈-6-O-β-D-葡萄糖苷(9)、3-[2′-(5′-羟甲基)呋喃基]-1(2H)-异喹啉酮-7-O-β-D-葡萄糖苷(10)。结论化合物2、4、7、8、10为首次从菘蓝属植物中分离得到。化合物10具有明显的抗HSV-2型病毒作用,治疗指数(TI)为6.07;化合物1、5、6对HSV病毒也表现出一定的抑制作用。

Objective To study the chemical constituents in the antiviral fraction of Isatidis Radix and the activity of the monomer components. Methods The water extract of lsatidis Radix was adsorbed by macroporous resin, and the antiviral fraction was eluted with 10% and 50% ethanol, repeatedly separated and purificated by silica gel column chromatography, reverse phase silica gel column chromatography, and Sephadex LH-20. The chemical structures were identificated using physicochemical constants and spectral data. Results Ten compounds were isolated from the active fraction of water extract, and they were respectively identified as syringin （1）, 4-（1, 2, 3-trihydroxypropyl）-2, 6-dimethoxyphenyl1-O-β-D-glucopyranoside （2）, isolariciresino （3）, isolariciresinol 4-O-[t-D- glucopyranoside （4）, lariciresinol-4-O-β-D-glucopyranoside （5）, lariciresinol-4, 4＇-bis-O-β-D-glucopyranoside （6）, 2-hydroxy-1, 4-benzenedi carboxylic acid （7）, D-mannitol （8）, indole-3-acetonitrile6-O-β-D-glucopyranoside （9）, and 3-[2＇-（5＇-hydroxymethyl） furyl]-1（2H）-isoquinoline-7-O-β-D-glucopyranoside （10）. Conclusion Compounds 2, 4, 7, 8, and 10 are isolated from lsatidis Radix for the first time. Compound 10 has the significant effect of anti-HSV-2 virus. Therapeutic index （TI） is 6.07. Compounds 1, 5, and 6 also show some inhibition to HSV virus.