贯叶金丝桃化学成分研究

目的:研究贯叶金丝桃Hypericum perforatum的化学成分。方法:通过各种柱色谱进行分离纯化,根据理化性质和波谱数据对所得化合物进行结构鉴定;测定化合物对基因重组人PTP1B的抑制率。结果:从中分离并鉴定了10个化合物:D-甘露醇(1),邻苯二甲酸二异丁酯(2),(7E,6R,9S)-9-hydroxy-4,7-megastigmadien-3-one(3),(6S,9R)-roseoside(4),2,6-dim-ethoxy-4-hydroquinone-1-O-β-D-glucopyranoside(5),2,6-dimethoxy-4-hydroxybenzyl alcohol 1-O-β-D-glucopyranoside(6),syringate4-O-β-glucopyranoside(7),金丝桃素(8),skyrin-6-O-β-D-glucopyranoside(9),(R)-3,4-二羟基-苯甲酸-1’-丙三醇酯(10)。在2μmol.L-1时,化合物9对基因重组人PTP1B的抑制率为96.4%,IC50为2.5μmol.L-1。结论:化合物10为新化合物,化合物2～4,7为首次从该属中分离得到,化合物5,6从该植物中首次得到。体外活性筛选表明化合物8具有显著的PTP1B抑制作用。

Chemical constituents from Hypericum perforatum

Objective: To study the chemical constituents from Hypericum perforatum.Method: Compouds were isolated by chromatographic techniques.Their structures were identified by spectral methods.The inhibitory activity of recombinant human PTP1B was evaluated.Result: Nine compounds were elucidated as D-Mannitol(1),1,2-benzenedicarboxylic acid bis(1-methylpropyl) ester(2),(7E,6R,9S)-9-hydroxy-4,7-megastigmadien-3-one(3),(6S,9R)-roseoside(4),2,6-dimethoxy-4-hydroquinone-1-O-β-Dglucopyranoside(5),2,6-di-methoxy-4-hydroxybenzyl alcohol 1-O-β-D-glucopyranoside(6),syringate 4-O-β-glucopyranoside(7),hypericin(8),skyrin-6-O-β-D-glucopyranoside(9),(R)-2,3-dihydroxypropyl 3,4-dihydroxy-benzoate(10).At a concentration of 2 μmol.L-1,compound 8 inhibited recombinant human PTP1B with inhibitory rate of 96.4% and IC50 of 2.5 μmol.L-1.Conclusion: compound 10 was new,compounds 2-4,7 were obtained from Hypericum for the first time and compounds 5-6 was isolated from this plant for the first time.Compound 8 showed remarkable PTP1B inhibitory activity.