Novel pyran-based anti-inflammatory agents: design, synthesis, and mechanistic studies in LPS-stimulated macrophages
Abstract This study investigated the anti-inflammatory effects of pyran derivatives, focusing on compound 19, in LPS-stimulated RAW264.7 macrophages. We screened 19 pyran derivatives for cytotoxicity and nitric oxide (NO) inhibition, and identified compound 19 as the most promising compound owing to...
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| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
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SpringerOpen
2025-08-01
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| Series: | Applied Biological Chemistry |
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| Online Access: | https://doi.org/10.1186/s13765-025-01018-5 |
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| author | Mei Tong He Sung Jin Kim Viet Duc Le Su Ji Min Heesu Lee Jae Wook Lee Myoung-Sook Shin |
| author_facet | Mei Tong He Sung Jin Kim Viet Duc Le Su Ji Min Heesu Lee Jae Wook Lee Myoung-Sook Shin |
| author_sort | Mei Tong He |
| collection | DOAJ |
| description | Abstract This study investigated the anti-inflammatory effects of pyran derivatives, focusing on compound 19, in LPS-stimulated RAW264.7 macrophages. We screened 19 pyran derivatives for cytotoxicity and nitric oxide (NO) inhibition, and identified compound 19 as the most promising compound owing to its efficacy. Western blot analysis revealed that compound 19 significantly inhibited the expression of key inflammatory mediators such as inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 in LPS-stimulated macrophages in a dose-dependent manner. Furthermore, compound 19 inhibited the phosphorylation of Akt at 12.5 μM, and suppressed JNK and ERK MAPK phosphorylation at both concentrations (12.5 and 6.25 μM), while p38 phosphorylation was not inhibited. These findings suggest that compound 19 exerts its anti-inflammatory action by modulating multiple signaling pathways involved in inflammatory responses. Our results demonstrate that compound 19 is a promising candidate for the development of novel anti-inflammatory agents. |
| format | Article |
| id | doaj-art-3a1d13b5d9c948ee8103337b8f9fc7dd |
| institution | Kabale University |
| issn | 2468-0842 |
| language | English |
| publishDate | 2025-08-01 |
| publisher | SpringerOpen |
| record_format | Article |
| series | Applied Biological Chemistry |
| spelling | doaj-art-3a1d13b5d9c948ee8103337b8f9fc7dd2025-08-20T03:43:10ZengSpringerOpenApplied Biological Chemistry2468-08422025-08-0168111010.1186/s13765-025-01018-5Novel pyran-based anti-inflammatory agents: design, synthesis, and mechanistic studies in LPS-stimulated macrophagesMei Tong He0Sung Jin Kim1Viet Duc Le2Su Ji Min3Heesu Lee4Jae Wook Lee5Myoung-Sook Shin6College of Korean Medicine, Gachon UniversityCollege of Korean Medicine, Gachon UniversityNatural Product Research Center, Korea Institute of Science and Technology (KIST)College of Korean Medicine, Gachon UniversityDepartment of Anatomy, College of Dentistry, Gangneung Wonju National UniversityNatural Product Research Center, Korea Institute of Science and Technology (KIST)College of Korean Medicine, Gachon UniversityAbstract This study investigated the anti-inflammatory effects of pyran derivatives, focusing on compound 19, in LPS-stimulated RAW264.7 macrophages. We screened 19 pyran derivatives for cytotoxicity and nitric oxide (NO) inhibition, and identified compound 19 as the most promising compound owing to its efficacy. Western blot analysis revealed that compound 19 significantly inhibited the expression of key inflammatory mediators such as inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 in LPS-stimulated macrophages in a dose-dependent manner. Furthermore, compound 19 inhibited the phosphorylation of Akt at 12.5 μM, and suppressed JNK and ERK MAPK phosphorylation at both concentrations (12.5 and 6.25 μM), while p38 phosphorylation was not inhibited. These findings suggest that compound 19 exerts its anti-inflammatory action by modulating multiple signaling pathways involved in inflammatory responses. Our results demonstrate that compound 19 is a promising candidate for the development of novel anti-inflammatory agents.https://doi.org/10.1186/s13765-025-01018-5InflammationPyran derivativesMAPKs |
| spellingShingle | Mei Tong He Sung Jin Kim Viet Duc Le Su Ji Min Heesu Lee Jae Wook Lee Myoung-Sook Shin Novel pyran-based anti-inflammatory agents: design, synthesis, and mechanistic studies in LPS-stimulated macrophages Applied Biological Chemistry Inflammation Pyran derivatives MAPKs |
| title | Novel pyran-based anti-inflammatory agents: design, synthesis, and mechanistic studies in LPS-stimulated macrophages |
| title_full | Novel pyran-based anti-inflammatory agents: design, synthesis, and mechanistic studies in LPS-stimulated macrophages |
| title_fullStr | Novel pyran-based anti-inflammatory agents: design, synthesis, and mechanistic studies in LPS-stimulated macrophages |
| title_full_unstemmed | Novel pyran-based anti-inflammatory agents: design, synthesis, and mechanistic studies in LPS-stimulated macrophages |
| title_short | Novel pyran-based anti-inflammatory agents: design, synthesis, and mechanistic studies in LPS-stimulated macrophages |
| title_sort | novel pyran based anti inflammatory agents design synthesis and mechanistic studies in lps stimulated macrophages |
| topic | Inflammation Pyran derivatives MAPKs |
| url | https://doi.org/10.1186/s13765-025-01018-5 |
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