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阿魏酸乙酯衍生物的合成及细胞毒性活性作为有效的抗炎剂。

Synthesis and cytotoxic activity of ethyl ferulate derivatives as potent anti-inflammatory agents.

机构信息

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.

出版信息

Nat Prod Res. 2024 Jan-Feb;38(2):261-269. doi: 10.1080/14786419.2022.2118739. Epub 2022 Sep 2.

DOI:10.1080/14786419.2022.2118739
PMID:36054816
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 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.

摘要

虽然目前有一系列的药理学制剂被用于缓解炎症,但这些抗炎药物中的许多在临床上的应用都伴随着很高的不良反应率,这使得它们不适合长期使用。因此,开发新型抗炎药物至关重要。天然化合物和衍生物,如阿魏酸乙酯,由于其结构多样性和广泛的生物活性,已成为许多药物发现工作的基础。在本研究中,合成了 24 种阿魏酸乙酯衍生物。使用 RAW264.7 细胞和 CCK-8、ELISA 和 Western blot 测定法评估了它们的抗炎活性。这些分析表明,大多数合成化合物表现出中等至高度的抗炎活性。特别是 c10 和 c23 对通过靶向 NF-κB 和 MAPK 信号通路抑制 RAW264.7 细胞产生肿瘤坏死因子-α的活性比阿魏酸乙酯或地塞米松更强,这表明这些化合物值得进一步研究。

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