Novel 2-phenyl-4H-chromen derivatives: synthesis and anti-inflammatory activity evaluation in vitro and in vivo
It is significant to design, synthesise and optimise flavonoid derivatives with better anti-inflammatory activity. This study aims to design and synthesise a series of novel 2-phenyl-4H-chromen-4-one compounds with anti-inflammatory; among them, compound 8 was discovered as the best one. And then, t...
| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Taylor & Francis Group
2022-12-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
| Subjects: | |
| Online Access: | https://www.tandfonline.com/doi/10.1080/14756366.2022.2124983 |
| _version_ | 1798031825424089088 |
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| author | Yun Xiao Yaoyao Yan Juncheng Du Xiaoxiao Feng Famin Zhang Xu Han Yong Hu Xinhua Liu |
| author_facet | Yun Xiao Yaoyao Yan Juncheng Du Xiaoxiao Feng Famin Zhang Xu Han Yong Hu Xinhua Liu |
| author_sort | Yun Xiao |
| collection | DOAJ |
| description | It is significant to design, synthesise and optimise flavonoid derivatives with better anti-inflammatory activity. This study aims to design and synthesise a series of novel 2-phenyl-4H-chromen-4-one compounds with anti-inflammatory; among them, compound 8 was discovered as the best one. And then, the effects of compound 8 on the TLR4/MAPK signalling pathway was carried out in vivo, the results indicated that compound 8 could downregulate NO, IL-6, and TNF-α expression, and suppress LPS-induced inflammation by inhibiting the TLR4/MAPK pathways. Furthermore, compound 8 reduced inflammation by a mouse model of LPS-induced inflammatory disease in vivo. The results suggest that compound 8 has the potential against inflammation through regulating TLR4/MAPK pathway and can be assessed further for drug development. |
| first_indexed | 2024-04-11T20:03:48Z |
| format | Article |
| id | doaj.art-a6a510922c844c969d52f4b55b311e22 |
| institution | Directory Open Access Journal |
| issn | 1475-6366 1475-6374 |
| language | English |
| last_indexed | 2024-04-11T20:03:48Z |
| publishDate | 2022-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj.art-a6a510922c844c969d52f4b55b311e222022-12-22T04:05:29ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742022-12-013712589259710.1080/14756366.2022.2124983Novel 2-phenyl-4H-chromen derivatives: synthesis and anti-inflammatory activity evaluation in vitro and in vivoYun Xiao0Yaoyao Yan1Juncheng Du2Xiaoxiao Feng3Famin Zhang4Xu Han5Yong Hu6Xinhua Liu7School of Pharmacy, Inflammation and Immune Mediated Diseases Laboratory of Anhui Province, Anhui Medical University, Hefei, P. R. ChinaSchool of Pharmacy, Inflammation and Immune Mediated Diseases Laboratory of Anhui Province, Anhui Medical University, Hefei, P. R. ChinaSchool of Pharmacy, Inflammation and Immune Mediated Diseases Laboratory of Anhui Province, Anhui Medical University, Hefei, P. R. ChinaSchool of Pharmacy, Inflammation and Immune Mediated Diseases Laboratory of Anhui Province, Anhui Medical University, Hefei, P. R. ChinaSchool of Pharmacy, Inflammation and Immune Mediated Diseases Laboratory of Anhui Province, Anhui Medical University, Hefei, P. R. ChinaSchool of Pharmacy, Inflammation and Immune Mediated Diseases Laboratory of Anhui Province, Anhui Medical University, Hefei, P. R. ChinaAnhui Academy of Agricultural Sciences, Agricultural Products Processing Institute, Hefei, P. R. ChinaSchool of Pharmacy, Inflammation and Immune Mediated Diseases Laboratory of Anhui Province, Anhui Medical University, Hefei, P. R. ChinaIt is significant to design, synthesise and optimise flavonoid derivatives with better anti-inflammatory activity. This study aims to design and synthesise a series of novel 2-phenyl-4H-chromen-4-one compounds with anti-inflammatory; among them, compound 8 was discovered as the best one. And then, the effects of compound 8 on the TLR4/MAPK signalling pathway was carried out in vivo, the results indicated that compound 8 could downregulate NO, IL-6, and TNF-α expression, and suppress LPS-induced inflammation by inhibiting the TLR4/MAPK pathways. Furthermore, compound 8 reduced inflammation by a mouse model of LPS-induced inflammatory disease in vivo. The results suggest that compound 8 has the potential against inflammation through regulating TLR4/MAPK pathway and can be assessed further for drug development.https://www.tandfonline.com/doi/10.1080/14756366.2022.21249832-Phenyl-4H-chromen-4-one derivativesanti-inflammatoryTLR4/MAPK pathway |
| spellingShingle | Yun Xiao Yaoyao Yan Juncheng Du Xiaoxiao Feng Famin Zhang Xu Han Yong Hu Xinhua Liu Novel 2-phenyl-4H-chromen derivatives: synthesis and anti-inflammatory activity evaluation in vitro and in vivo Journal of Enzyme Inhibition and Medicinal Chemistry 2-Phenyl-4H-chromen-4-one derivatives anti-inflammatory TLR4/MAPK pathway |
| title | Novel 2-phenyl-4H-chromen derivatives: synthesis and anti-inflammatory activity evaluation in vitro and in vivo |
| title_full | Novel 2-phenyl-4H-chromen derivatives: synthesis and anti-inflammatory activity evaluation in vitro and in vivo |
| title_fullStr | Novel 2-phenyl-4H-chromen derivatives: synthesis and anti-inflammatory activity evaluation in vitro and in vivo |
| title_full_unstemmed | Novel 2-phenyl-4H-chromen derivatives: synthesis and anti-inflammatory activity evaluation in vitro and in vivo |
| title_short | Novel 2-phenyl-4H-chromen derivatives: synthesis and anti-inflammatory activity evaluation in vitro and in vivo |
| title_sort | novel 2 phenyl 4h chromen derivatives synthesis and anti inflammatory activity evaluation in vitro and in vivo |
| topic | 2-Phenyl-4H-chromen-4-one derivatives anti-inflammatory TLR4/MAPK pathway |
| url | https://www.tandfonline.com/doi/10.1080/14756366.2022.2124983 |
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