林产化学与工业2024，Vol.44Issue(4)：61-69,9.DOI:10.3969/j.issn.0253-2417.2024.04.008
葛根素衍生物的设计合成及其对酪氨酸酶的激活作用研究
Design and Synthesis of Puerarin Derivatives and Their Activation Effects on Tyrosinase
摘要
Abstract
Eight puerarin derivatives(PD1-PD8)were designed and synthesized from puerarin,and their chemical structures were determined by mass spectrometry and nuclear magnetic resonance hydrogen spectroscopy.The activation activity of each derivative on tyrosinase was measured using the method of tyrosinase dopa rate oxidation.Molecular docking simulations were utilized to explore the binding mechanism of each derivative with tyrosinase.Enzyme kinetic analysis was performed to determine the type of activation.The structures of 8 puerarin derivatives were identified as:4'-methoxy-puerarin(PD1),4'-ethoxy-puerarin(PD2),4'-propoxyl-puerarin(PD3),7-O-acetyl-puerarin(PD4),7-O-trimethylacetyl-puerarin(PD5),7-methoxy-puerarin(PD6),7-O-ethoxycarbonylmethylene-puerarin(PD7),7,4'-O-diethoxycarbonylmethylene-puerarin(PD8).Enzyme kinetic results showed that PD6 were mixed activation types.The results of activation activity assay showed that PD6 was mixed activation,and the half activation concentration of PD6(EC50=0.416 mmol/L)was higher than that of puerarin(EC50=0.434 mmol/L).关键词
葛根素衍生物/合成/酪氨酸酶激活剂/动力学分析Key words
puerarin derivatives/synthesis/tyrosinase activator/kinetic analysis分类
化学化工引用本文复制引用
朱号天,宋科,于华忠,贺健,刘诗马,郭婕..葛根素衍生物的设计合成及其对酪氨酸酶的激活作用研究[J].林产化学与工业,2024,44(4):61-69,9.基金项目
国家自然科学基金资助项目(32060326) （32060326）
