新型取代苯乙醇葡萄糖氧苷的合成及其抗缺氧活性

以取代苯甲醛为原料，经Wittig反应、水解反应和NaBH₄还原反应制得5个取代苯乙醇衍生物（4a~4e）;以4a~4e和其他芳乙醇（4f~4r）为原料，依次与全乙酰化溴代葡萄糖经Koenigs-Knorr偶联和MeONa/MeOH脱除乙酰保护基，合成了18个取代苯乙醇葡萄糖氧苷类似物（5a~5r，其中5b~5r为新化合物），其结构经¹H NMR和HR-MS（ESI）表征。采用MTT法研究了5a~5r对缺氧损伤的内皮细胞（EA.hy926）代谢活力的影响。结果表明：5e, 5g, 5m, 5p, 5q和5r对EA.hy926的保护作用优于红景天苷。

Synthesis of Novel Substituted Phenylethanol O-glycosides and Their Anti-hypoxic Activities

Five substituted phenylethanol derivatives(4a~4e) were obtained by Wittig reaction, hydrolysis reaction and NaBH4 reduction from substituted benzaldehydes.Eighteen substituted phenylethanol O-glycosides(5a~5r, among them 5b~5r were novel compounds) were synthesized by Koenigs-Knorr reaction following by deacetylation from fully acetylated glucopyranose bromide and substituted phenylethanol derivatives(4a~4r).The structures were characterized by 1H NMR and HR-MS(ESI).The anti-hypoxic activities of 5a~5r on endothelial cells(EA.hy926) exposed to hypoxia were investigated by MTT assays.The results indicated that 5e, 5g, 5m, 5p, 5q and 5r exhibited better anti-hypoxic activities than salidroside on EA.hy926.