【摘要】 目的设计并合成白藜芦醇的多种糖苷衍生物,测定其与全反式维甲酸(ATRA)联合用药后对人类急性早幼粒细胞白血病细胞株(NB4)的诱导分化作用。方法应用保护基策略,采用Schmidt成苷法制得目标产物;采用NBT还原法测定细胞分化百分率。结果与结论合成了10个白藜芦醇的单糖苷化衍生物,其中,Res-3-Rha、Res-4′-Rha、Res-4′-Xyl、Res-4′-Ara是未见文献报道的新化合物;Res-3-Xyl和Res-3-Ara为首次合成的化合物,其结构均经核磁共振氢谱和质谱确证。白藜芦醇及其10个糖苷衍生物与ATRA的联合给药初筛结果表明,Res-3-Glc、Res-3-Ara、Res-3-Rha、Res-4′-Glc、Res-4′-Ara、Res-4′-Xyl及5μmol.L-1的白藜芦醇和Res-4′-Rha均能明显提高ATRA的诱导细胞分化活性。更多还原

【Abstract】 Aim To find novel resveratrol glycosides with differentiation effects of NB4 cells after combining administration with all-trans retinoic acid(ATRA).Methods The target compounds were synthesized by Schmidt’s glycosidation method,and were screened by NBT reduction assay.Results and conclusion Ten resveratrol glycoside derivatives were synthesized,including four new compounds Res-3-Rha,Res-4’-Rha,Res-4’-Xyl,Res-4’-Ara and two firstly synthesized compounds Res-3-Xyl and Res-3-Ara,and their structures were identified by 1H-NMR and ESI-MS.The differentiation rates of groups treated with combination of ATRA with Res-3-Glc,Res-4’-Glc,Res-4’-Xyl,Res-3-Ara,Res-4’-Ara,Res-3-Rha at the concentration of 5 μmol·L-1 and 10 μmol·L-1,and resveratrol,Res-4’-Rha at the concentration of 5 μmol·L-1 were significantly higher than those treated with the same dose of ATRA alone.更多还原