Autor: |
Fu DN; Medicinal Chemistry and Pharmacology Institute, Inner Mongolia Minzu University, Tongliao, Inner Mongolia, P.R. China.; Inner Mongolia Key Laboratory of Mongolian Medicine Pharmacology for Cardio-Cerebral Vascular System, Tongliao, Inner Mongolia, P.R. China., Kong ZY; Medicinal Chemistry and Pharmacology Institute, Inner Mongolia Minzu University, Tongliao, Inner Mongolia, P.R. China.; Inner Mongolia Key Laboratory of Mongolian Medicine Pharmacology for Cardio-Cerebral Vascular System, Tongliao, Inner Mongolia, P.R. China., Sun W; Medicinal Chemistry and Pharmacology Institute, Inner Mongolia Minzu University, Tongliao, Inner Mongolia, P.R. China.; Inner Mongolia Key Laboratory of Mongolian Medicine Pharmacology for Cardio-Cerebral Vascular System, Tongliao, Inner Mongolia, P.R. China., Bai CM; Medicinal Chemistry and Pharmacology Institute, Inner Mongolia Minzu University, Tongliao, Inner Mongolia, P.R. China.; Inner Mongolia Key Laboratory of Mongolian Medicine Pharmacology for Cardio-Cerebral Vascular System, Tongliao, Inner Mongolia, P.R. China., Wu Y; Affiliated Hospital of Inner Mongolia Minzu University, Tongliao, Inner Mongolia, P.R. China., Bian M; Medicinal Chemistry and Pharmacology Institute, Inner Mongolia Minzu University, Tongliao, Inner Mongolia, P.R. China.; Inner Mongolia Key Laboratory of Mongolian Medicine Pharmacology for Cardio-Cerebral Vascular System, Tongliao, Inner Mongolia, P.R. China., Ma QQ; Medicinal Chemistry and Pharmacology Institute, Inner Mongolia Minzu University, Tongliao, Inner Mongolia, P.R. China.; Inner Mongolia Key Laboratory of Mongolian Medicine Pharmacology for Cardio-Cerebral Vascular System, Tongliao, Inner Mongolia, P.R. China. |
Abstrakt: |
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. |