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Research Article | Open Access

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

Xiangxin Lia,1, Yijing Pua,b,1, Haitao Jiangb, Wenxiao Jiaoc, Wenjun Penga,1, Wenli Tiana,1, Weibo Jiangb( ), Xiaoming Fanga ( )
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
College of Food Science and Engineering, Qilu University of Technology (Shandong Academy of Sciences), Jinan 250353, China

1 These authors contributed equally to this work.

Peer review under responsibility of Tsinghua University Press.

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Highlights

• The interaction between inhibitors and CEase was exothermic and spontaneous process.

• The interaction occurred through non-covalent interaction.

• Tannins inhibited the activity of CEase by changing the conformations of CEase.

• The interaction appeared as a key mechanism to influence cholesterol metabolism.

• The combination of PC/TA and orlistat showed a synergetic inhibition effect on CEase.

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 verif ied 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.

Graphical Abstract

Keywords

Cholesterol esterasePolyphenolsInteraction mechanismsMolecular dynamic simulationSynergistic effect

References

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Food Science and Human Wellness
Volume 13 Issue 1,
January 2024
Pages 360-369
DOI: 10.26599/FSHW.2022.9250030

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Li X, Pu Y, Jiang H, et al. Inhibitory effect of procyanidin B2 and tannin acid on cholesterol esterase and their synergistic effect with orlistat. Food Science and Human Wellness, 2024, 13(1): 360-369. https://doi.org/10.26599/FSHW.2022.9250030

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Received: 07 April 2022
Revised: 17 May 2022
Accepted: 04 July 2022
Published: 01 June 2023
© 2024 Beijing Academy of Food Sciences. Publishing services by Tsinghua University Press.

This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).