白藜芦醇类似物的合成及抗糖尿病活性

Synthesis of resveratrol analogues and evaluation of their anti⁃diabetic activity

目的:合成白藜芦醇类似物,考察其抗糖尿病活性及作用机制。方法:以不同取代的苯胺和不同取代的苯甲醛为原料,在乙醇回流下合成了白藜芦醇类似物,并测试其在棕榈酸(palmitic acid,PA)刺激下对胰岛β细胞的保护作用,同时探究优势化合物抗糖尿病的作用机制。结果:大部分化合物在PA刺激下对胰岛β细胞有保护作用,化合物JA10和JA12具有明显的细胞保护作用。分子机制研究显示,化合物JA10和JA12可以减少PA刺激下细胞内活性氧的生成,同时可以抑制炎症因子IL⁃1β和IL⁃6的基因表达。结论:白藜芦醇类似物JA10和JA12是潜在的抗糖尿病新化学实体。

Objective:To synthesize resveratrol analogues and investigate their anti⁃diabetic activity and related mechanism.Methods:Using different substituted anilines and different substituted benzaldehydes as raw materials,resveratrol analogs were synthesized under ethanol reflux,and their protective effects on pancreaticβcells were tested under the stimulation of palmitic acid(PA).The anti⁃diabetic mechanism of the dominant compounds was explored.Results:Most of the compounds have protective effects on pancreaticβcells,and the compounds JA10 and JA12 have significant cytoprotective effects.Molecular mechanism studies showed that the compounds JA10 and JA12 reduced the generation of reactive oxygen,and inhibited the gene expression of inflammatory factors IL⁃1βand IL⁃6.Conclusion:The resveratrol analogs JA10 and JA12 are potential antidiabetic new chemical entities.