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

Xiangxin Li ¹Yijing Pu ²Haitao Jiang ³Wenxiao Jiao ⁴Wenjun Peng ¹Wenli Tian ¹Weibo Jiang ³Xiaoming Fang¹

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作者信息

1. Institute of Apicultural Research,Chinese Academy of Agricultural Sciences,Beijing 100093,China
2. Institute of Apicultural Research,Chinese Academy of Agricultural Sciences,Beijing 100093,China;College of Food Science and Nutritional Engineering,China Agricultural University,Beijing 100083,China
3. College of Food Science and Nutritional Engineering,China Agricultural University,Beijing 100083,China
4. College of Food Science and Engineering,Qilu University of Technology(Shandong Academy of Sciences),Jinan 250353,China
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Abstract

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,UV-vis 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.

Key words

Cholesterol esterase/Polyphenols/Interaction mechanisms/Molecular dynamic simulation/Synergistic effect

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基金项目

国家重点基础研究发展计划(973计划)('973'program)

国家重点基础研究发展计划(973计划)(2013CB127106)

出版年

2024

食品科学与人类健康(英文)

CSTPCDCSCD

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参考文献量45

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