目的 制备新的七叶皂苷衍生物。方法 采用β-葡萄糖苷酶对娑罗子提取物进行生物转化，采用大孔吸附树脂、反相硅胶柱色谱等分离方法对酶解产物进行分离纯化，根据MS、NMR数据，对得到的单体化合物进行了结构鉴定。结果 4个化合物分别鉴定为21β-O-巴豆酰基-22α-O-乙酰基原七叶皂苷元-3β-O-[β-D-葡萄糖基(1→2)]-β-D-葡萄糖醛酸苷（1）、21β-O-当归酰基-22α-O-乙酰基原七叶皂苷元-3β-O-[β-D-葡萄糖基(1→2)]-β-D-葡萄糖醛酸苷（2）、21β-O-巴豆酰基-28-O-乙酰基原七叶皂苷元-3β-O-[β-D-葡萄糖基(1→2)]-β-D-葡萄糖醛酸苷（3）、21β-O-当归酰基-28-O-乙酰基原七叶皂苷元-3β-O-[β-D-葡萄糖基(1→2)]-β-D-葡萄糖醛酸苷（4）。分别命名为七叶皂苷Ie、七叶皂苷If、异七叶皂苷Ie和异七叶皂苷If。结论 4个化合物均为新化合物。

Objective To prepare new derivatives of aescine. Methods The biotransformation of Aesculi Semen extract was conducted with β-glucosidase. The macroporous adsorption resin and reverse phase silica gel column chromatography were used to isolate the zymolyte, and the structures of the monomer compounds were elucidated by MS and NMR. Results Four compounds were identified as 21β-O-tigloyl-22α-O-acetylprotoaescigenin-3β-O-[β-D-glucopyranosyl (1→2)]-β-D-glucopyranosiduronic acid (1), 21β- O-angeloyl-22α-O-acetylprotoaescigenin-3β-O-[β-D-glucopyranosyl(1→2)]-β-D-glucopyranosiduronic acid (2), 21β-O-tigloyl-28-O- acetylprotoaescigenin-3β-O-[β-D-glucopyranosyl (1→2)]-β-D-glucopyranosiduronic acid (3), and 21β-O-angeloyl-28-O- acetylprotoaescigenin- 3β-O-[β-D-glucopyranosyl(1→2)]-β-D-glucopyranosiduronic acid (4), and named escin Ie, escin If, isoescin Ie, and isoescin If, respectively. Conclusion Compound 1－4 are new products.

国家重大新药创制专项（2011ZX09401-009）