3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one inhibits allergic reactions in IgE-mediated RBL-2H3 cells and a passive cutaneous anaphylaxis mouse model
Abstract Allergic reactions occur when the immune system overreacts to generally harmless substances, leading to both acute and chronic diseases, which can be fatal. Mast cells are critical mediators of allergic reactions as they bind allergens and trigger the release of inflammatory mediators. In t...
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SpringerOpen
2025-01-01
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| Series: | Applied Biological Chemistry |
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| Online Access: | https://doi.org/10.1186/s13765-025-00979-x |
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| author | Moonsu Kim Huiji Kim Sun Young Moon Seong-Ah Shin Minji Kim Seyeon Choi Sugeun Gwon Jun Hyuck Lee Hyun Ho Park Chang Sup Lee |
| author_facet | Moonsu Kim Huiji Kim Sun Young Moon Seong-Ah Shin Minji Kim Seyeon Choi Sugeun Gwon Jun Hyuck Lee Hyun Ho Park Chang Sup Lee |
| author_sort | Moonsu Kim |
| collection | DOAJ |
| description | Abstract Allergic reactions occur when the immune system overreacts to generally harmless substances, leading to both acute and chronic diseases, which can be fatal. Mast cells are critical mediators of allergic reactions as they bind allergens and trigger the release of inflammatory mediators. In this study, we investigated the anti-allergic effects of the coumarin derivative 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one in rat basophilic leukemia (RBL)-2H3 cells sensitized to dinitrophenyl (DNP)-immunoglobulin E (IgE) and human serum albumin (HSA). Our results demonstrated that 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one effectively reduces the release of β-hexosaminidase and histamine, inhibiting mast cell degranulation. Additionally, 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one suppressed the production of allergy-related pro-inflammatory cytokines (IL-4, IL-13, and TNF-α) and inhibited key signaling pathways, including MAPK, AKT, and NF-κB. Furthermore, in a passive cutaneous anaphylaxis (PCA) mouse model, 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one reduced ear edema and Evans blue infiltration, further confirming its anti-allergic effects. Collectively, these findings suggest that 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one is a promising candidate for the development of anti-allergic therapeutics. |
| format | Article |
| id | doaj-art-6e20f790b0234c2a9164ea227485fce2 |
| institution | Kabale University |
| issn | 2468-0842 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | SpringerOpen |
| record_format | Article |
| series | Applied Biological Chemistry |
| spelling | doaj-art-6e20f790b0234c2a9164ea227485fce22025-01-12T12:36:47ZengSpringerOpenApplied Biological Chemistry2468-08422025-01-0168111110.1186/s13765-025-00979-x3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one inhibits allergic reactions in IgE-mediated RBL-2H3 cells and a passive cutaneous anaphylaxis mouse modelMoonsu Kim0Huiji Kim1Sun Young Moon2Seong-Ah Shin3Minji Kim4Seyeon Choi5Sugeun Gwon6Jun Hyuck Lee7Hyun Ho Park8Chang Sup Lee9Collage of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National UniversityCollage of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National UniversityCollage of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National UniversityCollage of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National UniversityCollage of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National UniversityCollage of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National UniversityCollage of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National UniversityResearch Unit of Cryogenic Novel Material, Korea Polar Research InstituteCollege of Pharmacy, Chung-Ang UniversityCollage of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National UniversityAbstract Allergic reactions occur when the immune system overreacts to generally harmless substances, leading to both acute and chronic diseases, which can be fatal. Mast cells are critical mediators of allergic reactions as they bind allergens and trigger the release of inflammatory mediators. In this study, we investigated the anti-allergic effects of the coumarin derivative 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one in rat basophilic leukemia (RBL)-2H3 cells sensitized to dinitrophenyl (DNP)-immunoglobulin E (IgE) and human serum albumin (HSA). Our results demonstrated that 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one effectively reduces the release of β-hexosaminidase and histamine, inhibiting mast cell degranulation. Additionally, 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one suppressed the production of allergy-related pro-inflammatory cytokines (IL-4, IL-13, and TNF-α) and inhibited key signaling pathways, including MAPK, AKT, and NF-κB. Furthermore, in a passive cutaneous anaphylaxis (PCA) mouse model, 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one reduced ear edema and Evans blue infiltration, further confirming its anti-allergic effects. Collectively, these findings suggest that 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one is a promising candidate for the development of anti-allergic therapeutics.https://doi.org/10.1186/s13765-025-00979-xAllergyMast cells3-Bromo-4-(2-Hydroxyethyl)-7-Methoxy-2H-Chromen-2-OneAnti-Allergic therapeuticsAKT pathwayMAPK pathway |
| spellingShingle | Moonsu Kim Huiji Kim Sun Young Moon Seong-Ah Shin Minji Kim Seyeon Choi Sugeun Gwon Jun Hyuck Lee Hyun Ho Park Chang Sup Lee 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one inhibits allergic reactions in IgE-mediated RBL-2H3 cells and a passive cutaneous anaphylaxis mouse model Applied Biological Chemistry Allergy Mast cells 3-Bromo-4-(2-Hydroxyethyl)-7-Methoxy-2H-Chromen-2-One Anti-Allergic therapeutics AKT pathway MAPK pathway |
| title | 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one inhibits allergic reactions in IgE-mediated RBL-2H3 cells and a passive cutaneous anaphylaxis mouse model |
| title_full | 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one inhibits allergic reactions in IgE-mediated RBL-2H3 cells and a passive cutaneous anaphylaxis mouse model |
| title_fullStr | 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one inhibits allergic reactions in IgE-mediated RBL-2H3 cells and a passive cutaneous anaphylaxis mouse model |
| title_full_unstemmed | 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one inhibits allergic reactions in IgE-mediated RBL-2H3 cells and a passive cutaneous anaphylaxis mouse model |
| title_short | 3-bromo-4-(2-hydroxyethyl)-7-methoxy-2H-chromen-2-one inhibits allergic reactions in IgE-mediated RBL-2H3 cells and a passive cutaneous anaphylaxis mouse model |
| title_sort | 3 bromo 4 2 hydroxyethyl 7 methoxy 2h chromen 2 one inhibits allergic reactions in ige mediated rbl 2h3 cells and a passive cutaneous anaphylaxis mouse model |
| topic | Allergy Mast cells 3-Bromo-4-(2-Hydroxyethyl)-7-Methoxy-2H-Chromen-2-One Anti-Allergic therapeutics AKT pathway MAPK pathway |
| url | https://doi.org/10.1186/s13765-025-00979-x |
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