1. Synthesis and cytotoxic activity of ethyl ferulate derivatives as potent anti-inflammatory agents.
- Author
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Fu, Dan-ni, Kong, Zi-yi, Sun, Wen, Bai, Chun-mei, Wu, Yun, Bian, Ming, and Ma, Qian-qian
- Subjects
ANTI-inflammatory agents ,DRUG discovery ,BIODIVERSITY ,CELLULAR signal transduction ,CHEMICAL synthesis ,DEXAMETHASONE - Abstract
While a range of pharmacological agents are currently used to alleviate inflammation, the clinical administration of many of these anti-inflammatory drugs is associated with high rates of adverse side effects that make them poorly suited to long-term use. Therefore, there is a critical need for the development of novel anti-inflammatory agents. Natural compounds and derivatives like ethyl ferulate have risen to prominence as a foundation for many drug discovery efforts owing to their structural diversity and wide-ranging biological activities. In the present study, 24 ethyl ferulate derivatives were synthesized. Their anti-inflammatory activity was evaluated in vitro using RAW264.7 cells and CCK-8, ELISA, and Western blotting assays. These analyses revealed that most of the synthesized compounds exhibited moderate to high anti-inflammatory activities. In particular, c10 and c23 exerted more pronounced activity than ethyl ferulate or dexamethasone with respect to the suppression of tumour necrosis factor-α production by RAW264.7 cells through the targeting of the NF-κB and MAPK signalling pathways, suggesting that these compounds warrant further investigation. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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