刘福俊, 王晓晶, 王芳, 王兴红, 杨丽娟, 黄超. 天然二氢查尔酮类衍生物的合成及降糖活性筛选[J]. 云南大学学报(自然科学版), 2020, 42(3): 545-552. doi: 10.7540/j.ynu.20190641
引用本文: 刘福俊, 王晓晶, 王芳, 王兴红, 杨丽娟, 黄超. 天然二氢查尔酮类衍生物的合成及降糖活性筛选[J]. 云南大学学报(自然科学版), 2020, 42(3): 545-552. doi: 10.7540/j.ynu.20190641
LIU Fu-jun, WANG Xiao-jing, WANG Fang, WANG Xing-hong, YANG Li-juan, HUANG Chao. Synthesis and hypoglycemic activity screening of natural dihydrochalcone derivatives[J]. Journal of Yunnan University: Natural Sciences Edition, 2020, 42(3): 545-552. DOI: 10.7540/j.ynu.20190641
Citation: LIU Fu-jun, WANG Xiao-jing, WANG Fang, WANG Xing-hong, YANG Li-juan, HUANG Chao. Synthesis and hypoglycemic activity screening of natural dihydrochalcone derivatives[J]. Journal of Yunnan University: Natural Sciences Edition, 2020, 42(3): 545-552. DOI: 10.7540/j.ynu.20190641

天然二氢查尔酮类衍生物的合成及降糖活性筛选

Synthesis and hypoglycemic activity screening of natural dihydrochalcone derivatives

  • 摘要: 从天然二氢查尔酮降糖物质出发,设计合成二氢查尔酮类衍生物并筛选其降糖活性. 以廉价易得的苯甲醛、苯乙酮衍生物为原料,经两步反应制得14个二氢查尔酮类化合物(其中 6 个新化合物),其结构经1H NMR、13C NMR、HRMS及IR表征. 以胰岛素为阳性对照药,通过脂肪细胞模型葡萄糖消耗量试验检测目标化合物的降血糖活性. 研究结果显示,新化合物 4n 降血糖活性最为显著,其葡萄糖消耗量为4.64 mmol·L−1,与正常组相比提高了13.11%. 文章为探讨二氢查尔酮化合物的制备和降糖构效关系提供了实验基础.

     

    Abstract: Based on the hypoglycemic activity of dihydrochalcone, dihydrochalcone derivatives were designed and synthesized, and their hypoglycemic activities were screened. Fourteen dihydrochalcone compounds (six of which are new compounds) were synthesized from inexpensive benzaldehyde and acetophenone derivatives. Their structures were characterized by 1H NMR, 13C NMR, HRMS and IR. The hypoglycemic activity of the target compound was detected by glucose consumption test of fat cell model with insulin as positive control. The results showed that the new compound 4n had the most significant hypoglycemic activity, and its glucose consumption was 4.64 mmol·L−1, which was 13.11% higher than that of the normal group. This paper provides the experimental basis for the preparation of dihydrochalcone compounds and the hypoglycemic structure-activity relationship.

     

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