Synthesis of urolithin derivatives and their anti-inflammatory activity
Copyright © 2024 Elsevier Inc. All rights reserved..
Two series of urolithin derivatives, totally 38 compounds, were synthesized. Their anti-inflammatory activity was investigated by detecting the inhibitory effects on the expression of TNF-α in bone marrow-derived macrophages (BMDMs), showing that 24 of 38 ones reduced the expression of TNF-α. Compound B2, the ring C opened derivative of urolithin B with a butoxycarbonyl substitution in ring A, showed the strongest inhibitory activity compared with that of indomethacin. Furthermore, B2 treatment decreased the expression of pro-inflammatory factors IL-1β, IL-6, iNOS and COX-2. Mechanically, the anti-inflammatory effect of B2 was related to the inhibition of NF-κB signaling pathway. These results clearly illustrated that B2 hold potential for application as an anti-inflammatory agent. The present study provided a viable approach to modify the gut metabolites for anti-inflammatory drug development.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:704 |
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| Enthalten in: |
Biochemical and biophysical research communications - 704(2024) vom: 16. März, Seite 149711 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Li, Xintong [VerfasserIn] |
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| Links: |
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| Themen: |
Anti-Inflammatory Agents |
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| Anmerkungen: |
Date Completed 13.03.2024 Date Revised 13.03.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.bbrc.2024.149711 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Two series of urolithin derivatives, totally 38 compounds, were synthesized. Their anti-inflammatory activity was investigated by detecting the inhibitory effects on the expression of TNF-α in bone marrow-derived macrophages (BMDMs), showing that 24 of 38 ones reduced the expression of TNF-α. Compound B2, the ring C opened derivative of urolithin B with a butoxycarbonyl substitution in ring A, showed the strongest inhibitory activity compared with that of indomethacin. Furthermore, B2 treatment decreased the expression of pro-inflammatory factors IL-1β, IL-6, iNOS and COX-2. Mechanically, the anti-inflammatory effect of B2 was related to the inhibition of NF-κB signaling pathway. These results clearly illustrated that B2 hold potential for application as an anti-inflammatory agent. The present study provided a viable approach to modify the gut metabolites for anti-inflammatory drug development | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Anti-inflammation activity | |
| 650 | 4 | |a NF-κB | |
| 650 | 4 | |a Structure-activity relationship | |
| 650 | 4 | |a Urolithin | |
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| 650 | 7 | |a Anti-Inflammatory Agents |2 NLM | |
| 650 | 7 | |a NF-kappa B |2 NLM | |
| 650 | 7 | |a Lipopolysaccharides |2 NLM | |
| 700 | 1 | |a Zhang, Zhengzheng |e verfasserin |4 aut | |
| 700 | 1 | |a Xu, Guangsen |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Zhiying |e verfasserin |4 aut | |
| 700 | 1 | |a Lu, Chunhua |e verfasserin |4 aut | |
| 700 | 1 | |a Shen, Yuemao |e verfasserin |4 aut | |
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