目的 制備新的七葉皂苷衍生物。方法 采用β-葡萄糖苷酶對(duì)娑羅子提取物進(jìn)行生物轉(zhuǎn)化，采用大孔吸附樹脂、反相硅膠柱色譜等分離方法對(duì)酶解產(chǎn)物進(jìn)行分離純化，根據(jù)MS、NMR數(shù)據(jù)，對(duì)得到的單體化合物進(jìn)行了結(jié)構(gòu)鑒定。結(jié)果 4個(gè)化合物分別鑒定為21β-O-巴豆?；?22α-O-乙?；呷~皂苷元-3β-O-[β-D-葡萄糖基(1→2)]-β-D-葡萄糖醛酸苷（1）、21β-O-當(dāng)歸?；?22α-O-乙?；呷~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?；?28-O-乙?；呷~皂苷元-3β-O-[β-D-葡萄糖基(1→2)]-β-D-葡萄糖醛酸苷（3）、21β-O-當(dāng)歸?；?28-O-乙酰基原七葉皂苷元-3β-O-[β-D-葡萄糖基(1→2)]-β-D-葡萄糖醛酸苷（4）。分別命名為七葉皂苷Ie、七葉皂苷If、異七葉皂苷Ie和異七葉皂苷If。結(jié)論 4個(gè)化合物均為新化合物。

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.

國(guó)家重大新藥創(chuàng)制專項(xiàng)（2011ZX09401-009）