Inhibitory effect of procyanidin B2 and tannin acid on cholesterol esterase and their synergistic effect with orlistat  

作　　者：Xiangxin Li Yijing Pu Haitao Jiang Wenxiao Jiao Wenjun Peng Wenli Tian Weibo Jiang Xiaoming Fang 

机构地区：[1]Institute of Apicultural Research,Chinese Academy of Agricultural Sciences,Beijing 100093,China [2]College of Food Science and Nutritional Engineering,China Agricultural University,Beijing 100083,China [3]College of Food Science and Engineering,Qilu University of Technology(Shandong Academy of Sciences),Jinan 250353,China

出　　处：《Food Science and Human Wellness》2024年第1期360-369,共10页食品科学与人类健康（英文）

基　　金：supported by the National Basic Research Program of China(‘973’program,2013CB127106)。

摘　　要：This study was aimed to analyze the effect of procyanidin B2(PC)and tannin acid(TA)on the activities of cholesterol esterase(CEase)and the inhibitory mechanisms of enzymatic activity.The interaction mechanisms were investigated by enzymatic kinetics,multi-spectroscopy methods,thermodynamics analysis,molecular docking,and dynamic simulations.PC and TA could bind with CEase and inhibit the activity of enzyme in a mixed-competitive manner and non-competitive manner,which was verified by molecular docking simulations and dynamics simulations.Also,PC and TA showed the synergistic inhibition with orlistat.Fluorescence,UVvis and the thermodynamic analysis revealed that the complexes were formed from CEase and inhibitors by noncovalent interaction.As revealed by the circular dichroism results,both PC and TA decreased enzymatic activities by altering the conformations of CEase.The inhibition of PC and TA on CEase might be one mechanism for its cholesterol-lowering effect.

关 键 词：Cholesterol esterase POLYPHENOLS Interaction mechanisms Molecular dynamic simulation Synergistic effect 

分 类 号：TQ460.1[化学工程—制药化工]