{"title":"A Natural Chalcone Cardamonin Inhibited Transformation of Aryl Hydrocarbon Receptor Through Binding to the Receptor Competitively","authors":"Tianshun Zhang, Chao He, Shieru Ota, Tomoya Kitakaze, Ryoichi Yamaji, Sayuri Shimazu, Yoko Yamashita, Hitoshi Ashida","doi":"10.1002/mnfr.202400185","DOIUrl":null,"url":null,"abstract":"<div>\n \n <section>\n \n <h3> Scope</h3>\n \n <p>Chalcones are widely present in most plants and have various health beneficial functions. This study investigates the suppressive effect of 13 natural and synthetic chalcones on transformation of aryl hydrocarbon receptor (AhR) induced by 2,3,7,8-tetrachlorodibenzo-<i>p</i>-dioxin (TCDD) and 3-methylcholanthrene (3-MC) in a cell-free system, Hepa-1c1c7 cells, and liver of ICR mice.</p>\n </section>\n \n <section>\n \n <h3> Methods and results</h3>\n \n <p>In the cell-free system, cardamonin dose-dependently inhibits AhR transformation. Chalcones with substitution on 2′ and/or 6′ position is important for the suppressive effect, while the substitution on 4′ position is negatively for the effect. Moreover, cardamonin and 2′-hydroxychalcone competitively inhibit the binding of [<sup>3</sup>H]-3-MC to the AhR. In Hepa-1c1c7 cells, cardamonin inhibits AhR transformation and expression of cytochrome P4501A1 (CYP1A1) in a dose-dependent manner through suppressing TCDD-induced phosphorylation of both AhR and AhR nuclear translocator, heterodimerization of them, and nuclear translocation of AhR. In the liver of mice, oral administered cardamonin also inhibits 3-MC-induced AhR translocation and expression of CYP1A1.</p>\n </section>\n \n <section>\n \n <h3> Conclusion</h3>\n \n <p>Among used chalcones, a natural chalcone cardamonin competitively binds to AhR and suppresses its transformation. Thus, cardamonin is an effective food factor for suppression of the dioxin-caused biochemical alterations and toxicities.</p>\n </section>\n </div>","PeriodicalId":212,"journal":{"name":"Molecular Nutrition & Food Research","volume":"68 18","pages":""},"PeriodicalIF":4.5000,"publicationDate":"2024-08-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Molecular Nutrition & Food Research","FirstCategoryId":"97","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/mnfr.202400185","RegionNum":2,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"FOOD SCIENCE & TECHNOLOGY","Score":null,"Total":0}
引用次数: 0
Abstract
Scope
Chalcones are widely present in most plants and have various health beneficial functions. This study investigates the suppressive effect of 13 natural and synthetic chalcones on transformation of aryl hydrocarbon receptor (AhR) induced by 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and 3-methylcholanthrene (3-MC) in a cell-free system, Hepa-1c1c7 cells, and liver of ICR mice.
Methods and results
In the cell-free system, cardamonin dose-dependently inhibits AhR transformation. Chalcones with substitution on 2′ and/or 6′ position is important for the suppressive effect, while the substitution on 4′ position is negatively for the effect. Moreover, cardamonin and 2′-hydroxychalcone competitively inhibit the binding of [3H]-3-MC to the AhR. In Hepa-1c1c7 cells, cardamonin inhibits AhR transformation and expression of cytochrome P4501A1 (CYP1A1) in a dose-dependent manner through suppressing TCDD-induced phosphorylation of both AhR and AhR nuclear translocator, heterodimerization of them, and nuclear translocation of AhR. In the liver of mice, oral administered cardamonin also inhibits 3-MC-induced AhR translocation and expression of CYP1A1.
Conclusion
Among used chalcones, a natural chalcone cardamonin competitively binds to AhR and suppresses its transformation. Thus, cardamonin is an effective food factor for suppression of the dioxin-caused biochemical alterations and toxicities.
期刊介绍:
Molecular Nutrition & Food Research is a primary research journal devoted to health, safety and all aspects of molecular nutrition such as nutritional biochemistry, nutrigenomics and metabolomics aiming to link the information arising from related disciplines:
Bioactivity: Nutritional and medical effects of food constituents including bioavailability and kinetics.
Immunology: Understanding the interactions of food and the immune system.
Microbiology: Food spoilage, food pathogens, chemical and physical approaches of fermented foods and novel microbial processes.
Chemistry: Isolation and analysis of bioactive food ingredients while considering environmental aspects.