查尔酮类衍生物的合成及其抑制酪氨酸酶活性评价  

Synthesis of Chalcone Derivatives and Evaluation of Their Inhibition of Tyrosinase Activity

作　　者：姜松周 吕金鹏 付莹 杨莹[1] 许煌 宋国强[1] JIANG Songzhou;LYU Jinpeng;FU Ying;YANG Ying;XU Huang;SONG Guoqiang(School of Pharmacy,Changzhou University,Changzhou 213164,China)

机构地区：[1]常州大学药学院,江苏常州213164

出　　处：《常州大学学报（自然科学版）》2021年第1期35-40,共6页Journal of Changzhou University：Natural Science Edition

摘　　要：以醛和酮为起始原料,合成了一系列查尔酮类衍生物(查尔酮、4-羟基查尔酮、异甘草素、甘草素),其结构经NMR表征。以这4种化合物为研究对象,L-酪氨酸为底物,蘑菇酪氨酸酶为催化剂,建立一个酪氨酸酶抑制剂的高通量筛选模型,经条件优化,最终选择L-酪氨酸的浓度为2.5 mmol/L,蘑菇酪氨酸酶的活性为2000 U/mL,反应时间为20 min。通过此模型对蘑菇酪氨酸酶的活性进行测定,来评价这4种化合物对酪氨酸酶活性的直接抑制作用,并筛选出了抑制率最高的化合物为异甘草素,从而为将来酪氨酸酶抑制剂的开发提供指导。A series of chalcone derivatives(chalcone,4-hydroxychalcone,isoliquiritigenin,glycyrrhizin)were synthesized using aldehydes and ketones as starting materials,and their structures were characterized by NMR.Using these four compounds as research objects,L-tyrosine as a substrate,and mushroom tyrosinase as a catalyst,a high-throughput screening model of tyrosinase inhibitors was established.After the optimization of conditions,the concentration of L-tyrosine was 2.5 mmol/L,the concentration of mushroom tyrosinase activity was 2000 U/mL,and the reaction time was 20 min.Through this model,the activity of mushroom tyrosinase was measured to evaluate the direct inhibition of tyrosinase activity by these four compounds,and the compound with the highest inhibition rate was screened for isoliquiritigenin to provide guidance for the development of tyrosinase inhibitors in future.

关 键 词：羟醛缩合 查尔酮 高通量筛选模型 蘑菇酪氨酸酶 抑制剂 

分 类 号：R914[医药卫生—药物化学]