Inhibitory effect of procyanidin B2 and tannin acid on cholesterol esterase and their synergistic effect with orlistat
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...
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| Format: | Article |
| Language: | English |
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Tsinghua University Press
2024-01-01
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| Series: | Food Science and Human Wellness |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2213453023001167 |
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| author | Xiangxin Li Yijing Pu Haitao Jiang Wenxiao Jiao Wenjun Peng Wenli Tian Weibo Jiang Xiaoming Fang |
| author_facet | Xiangxin Li Yijing Pu Haitao Jiang Wenxiao Jiao Wenjun Peng Wenli Tian Weibo Jiang Xiaoming Fang |
| author_sort | Xiangxin Li |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-8268778c5e6246af82d98ca22b7c7f03 |
| institution | Kabale University |
| issn | 2213-4530 |
| language | English |
| publishDate | 2024-01-01 |
| publisher | Tsinghua University Press |
| record_format | Article |
| series | Food Science and Human Wellness |
| spelling | doaj-art-8268778c5e6246af82d98ca22b7c7f032025-02-03T05:54:06ZengTsinghua University PressFood Science and Human Wellness2213-45302024-01-01131360369Inhibitory effect of procyanidin B2 and tannin acid on cholesterol esterase and their synergistic effect with orlistatXiangxin Li0Yijing Pu1Haitao Jiang2Wenxiao Jiao3Wenjun Peng4Wenli Tian5Weibo Jiang6Xiaoming Fang7Institute of Apicultural Research, Chinese Academy of Agricultural Sciences, Beijing 100093, ChinaInstitute of Apicultural Research, Chinese Academy of Agricultural Sciences, Beijing 100093, China; College of Food Science and Nutritional Engineering, China Agricultural University, Beijing 100083, ChinaCollege of Food Science and Nutritional Engineering, China Agricultural University, Beijing 100083, ChinaCollege of Food Science and Engineering, Qilu University of Technology (Shandong Academy of Sciences), Jinan 250353, ChinaInstitute of Apicultural Research, Chinese Academy of Agricultural Sciences, Beijing 100093, ChinaInstitute of Apicultural Research, Chinese Academy of Agricultural Sciences, Beijing 100093, ChinaCollege of Food Science and Nutritional Engineering, China Agricultural University, Beijing 100083, China; Corresponding authors. Fax: +86 010-82636445Institute of Apicultural Research, Chinese Academy of Agricultural Sciences, Beijing 100093, China; Corresponding authors. Fax: +86 010-82636445This 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.http://www.sciencedirect.com/science/article/pii/S2213453023001167Cholesterol esterasePolyphenolsInteraction mechanismsMolecular dynamic simulationSynergistic effect |
| spellingShingle | Xiangxin Li Yijing Pu Haitao Jiang Wenxiao Jiao Wenjun Peng Wenli Tian Weibo Jiang Xiaoming Fang Inhibitory effect of procyanidin B2 and tannin acid on cholesterol esterase and their synergistic effect with orlistat Food Science and Human Wellness Cholesterol esterase Polyphenols Interaction mechanisms Molecular dynamic simulation Synergistic effect |
| title | Inhibitory effect of procyanidin B2 and tannin acid on cholesterol esterase and their synergistic effect with orlistat |
| title_full | Inhibitory effect of procyanidin B2 and tannin acid on cholesterol esterase and their synergistic effect with orlistat |
| title_fullStr | Inhibitory effect of procyanidin B2 and tannin acid on cholesterol esterase and their synergistic effect with orlistat |
| title_full_unstemmed | Inhibitory effect of procyanidin B2 and tannin acid on cholesterol esterase and their synergistic effect with orlistat |
| title_short | Inhibitory effect of procyanidin B2 and tannin acid on cholesterol esterase and their synergistic effect with orlistat |
| title_sort | inhibitory effect of procyanidin b2 and tannin acid on cholesterol esterase and their synergistic effect with orlistat |
| topic | Cholesterol esterase Polyphenols Interaction mechanisms Molecular dynamic simulation Synergistic effect |
| url | http://www.sciencedirect.com/science/article/pii/S2213453023001167 |
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