槲皮素-3-O-乙酸-(4-硫代氨基)-苯酯的合成及其活性研究  

Synthesis and Activity Research of Quercetin-3-O-acetic acid-(4-thioamino)-phenyl Ester

作　　者：尚世康 黄晓江 刘建 何世波 金蝶 刘明星 SHANG Shikang;HUANG Xiaojiang;LIU Jian;HE Shibo;JIN Die;LIU Mingxing(School of Biological Engin.and Food,Hubei Univ.of Tech.,Wuhan 430068,China)

机构地区：[1]湖北工业大学生物工程与食品学院,湖北武汉430068

出　　处：《湖北工业大学学报》2024年第5期60-64,共5页Journal of Hubei University of Technology

基　　金：国家级大学生创新创业训练计划项目(202110500010)。

摘　　要：以芦丁为原料,以4-羟基硫代苯甲酰胺作为H_(2)S供体,合成一种抗糖尿病且促进伤口愈合的新型化合物槲皮素-3-O-乙酸-(4-硫代氨基)-苯酯。工艺路线包括取代、水解、williamson醚化、水解、还原和酯化,共6步反应,总收率4.6%。各步产物经MS、1H NMR分析表征。通过HUVECs细胞增殖实验、划痕实验以及胰岛素抵抗模型实验,验证该化合物不仅具有降糖作用,还具有促进糖尿病患者伤口愈合的功效。A novel compound quercetin-3-O-acetic acid-(4-thioamino)-phenyl ester,which is antidiabetic and promotes wound healing,was synthesized using rutin as raw material and 4-hydroxythiobenzamide as H_(2)S donor.The process route included substitution,hydrolysis,williamson etherification,hydrolysis,reduction and esterification in six steps with an overall yield of 4.6%.The products of each step were characterized by MS and 1H NMR analysis.The compounds were verified by HUVECs cell proliferation assay,scratch assay and insulin resistance model assay to have not only hypoglycemic effect,but also the efficacy of promoting wound healing in diabetic patients.

关 键 词：芦丁 H_(2)S供体 抗糖尿病药物 降糖作用 

分 类 号：O626.32[理学—有机化学]