目的 研究天目地黄Rehmannia chingii全草的化学成分。方法 通过正相硅胶、Sephadex LH-20以及反相HPLC柱等色谱方法对天目地黄的化学成分进行分离纯化,应用谱学技术鉴定化合物的结构。结果 从天目地黄水提取物中分离得到17个化合物,分别鉴定为8-甲基-9氢环戊烷并吡喃-1,3,6,8-四醇(1)、3,4-二羟基苯乙醇(2)、3-甲氧基-4-羟基苯乙醇(3)、苯乙醇-8-O-β-D-葡萄糖苷(4)、(3,4-二羟基苯乙醇)-鼠李糖-(1→3)-葡萄糖苷(5)、(苯乙醇)-木糖-(1→6)-葡萄糖苷(6)、去乙酰地黄苷(7)、毛蕊花糖苷(8)、异毛蕊花糖苷(9)、地黄苷(10)、异地黄苷(11)、焦地黄苯乙醇苷C(12)、焦地黄苯乙醇苷A₁(13)、焦地黄苯乙醇苷B₁(14)、3,4-dihydroxy-β-phenethyl-O-α-L-rhamnopyranosyl-(1→3)-O-β-D-galacopyranosyl-(1→6)-4-O-caffeoyl-β-D-glucopyranoside(15)、肉苁蓉苷F(16)、异肉苁蓉苷F(17)。结论 共鉴定17个化合物,包括1个环烯醚萜(1),16个苯乙醇及其苷(2~17);化合物1为新化合物,命名为天目地黄素;化合物16、17为首次从该属植物中分离得到。经体外活性筛选发现化合物9、12、14~16有醛糖还原酶抑制活性。

Objective To investigate the chemical constituents of Rehmannia chingii. Methods The compounds were isolated from an aqueous extract from the whole plants of R. chingii by a combination of various chromatographic techniques including column chromatography over silica gel and Sephadex LH-20 and reversed-phase HPLC. Their structures were identified by spectroscopic analysis including MS and NMR data. Results Seventeen compounds were isolated and identified as 8-methyloctahydrocyclopenta[c] pyran-1,3,6,8-tetraol (1), 3,4-dihydroxy-phenethyl alcohol (2), 3-methoxyl-4-hydroxyphenyl alcohol (3), phenylethyl-8-O-β-D-glucopyranoside (4), 3,4-dihydroxy-β-phenethyl-O-α-L-rhamnopyranosyl-(1→3)-O-β-D-glucopyranoside (5), 2-phenylethyl-O-β-D-xylopyranosyl-(1→6)-β-D-glucopyranoside (6), deacyl-martynoside (7), acteoside (8), isoacteoside (9), martynoside (10), isomartynoside (11), jionoside C (12), jionoside A₁ (13), jionoside B₁ (14), 3,4-dihydroxy-β-phenethyl-O-α-L-rhamnopyranosyl-(1→3)-O-β-D-galacopyranosyl-(1→6)-4-O-caffeoyl-β-D-glucopyranoside (15), cistanoside F (16), and isocistanoside F (17). Conclusion Among the isolated seventeen compounds, compound 1 is a new compound named rehmachinin, and compounds 16-17 are isolated from the plants of Rehmannia Libosch. ex Fisch. et Mey. for the first time. In the preliminary assays, compounds 9, 12, and 14-16 exhibit the obvious inhibition against aldose reductase.

国家自然科学基金资助项目(81403076)