Structural modification based on the diclofenac scaffold: Achieving reduced colitis side effects through COX-2/NLRP3 selective inhibition

Ju, Zhiran; Xu, Junde; Tang, Keshuang; Chen, Fener

doi:10.1016/j.ejmech.2024.116257

European Journal of Medicinal Chemistry

2024

DOI: 10.1016/j.ejmech.2024.116257

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Structural modification based on the diclofenac scaffold: Achieving reduced colitis side effects through COX-2/NLRP3 selective inhibition

Zhiran Ju,

Junde Xu,

Keshuang Tang

et al.

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Cited by 4 publications

References 39 publications

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Design, Synthesis and Biological Activities Evaluation of Novel Pterostilbene‐urea Derivatives as Potential Anti‐ inflammatory Agents

Wang,

Huang,

Peng

et al. 2024

Chemistry & Biodiversity

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To remove the toxicity of 10‐Pterostilbene methylamine hydrochloride derivatives (PMDS ． HCl) and develop novel anti‐inflammatory agents, twenty‐five Pterostilbene‐urea derivatives (PUDs, Q1‐Q25) derived from PMDs were designed, synthesized, characterized by spectroscopic techniques and their anti‐inflammatory activity in vitro were evaluated. Results exhibited that compounds (Q1‐Q25) were low toxic or non‐toxic toward RAW264.7 and L02 cell lines at 20 μM/L. Eight bioactive agents (Q4‐Q10, Q20) displayed obvious inhibition ability against LPS‐induced NO release, with IC50(NO) values ranged from 9.96 to 33.89 μM/L. Meanwhile, they were potential COX‐2 inhibitors with IC50(COX‐2) values ranging from 39.42 to 179.84 nM/L. A roughly positive correlation were observed between the inhibitory abilities on LPS‐induced NO release and those on COX‐2. Q7 , Q10and Q20 manifested stronger COX‐2 inhibitory abilities than Celecoxib . The strongest anti‐inflammatory agent, Q20 (IC50 (NO) = 9.96 μM/L, IC50(COX‐2) = 39.42 nM/L) effectively inhibited the secretion of pro‐inflammatory factors such as IL‐1β (IC50 = 12.30 μM/L) and TNF‐α (IC50 = 9.07 μM/L) in a dose‐dependent manner. Western Blot analysis indicated that at low micromolar concentrations, Q20 obviously down‐regulated the expression of COX‐2, iNOS as well as TLR4 protein, and suppressed the activation of NLRP3 inflammasome and NF‐κB signal pathway.

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Design, Synthesis and Biological Activities Evaluation of Novel Pterostilbene‐urea Derivatives as Potential Anti‐ inflammatory Agents

Wang,

Huang,

Peng

et al. 2024

Chemistry & Biodiversity

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show abstract

Potential COX-2 inhibitors modulating NF-κB/MAPK signaling pathways: Design, synthesis and evaluation of anti-inflammatory activity of Pterostilbene-carboxylic acid derivatives with an oxime ether moiety

Luo,

Chen,

Huang

et al. 2025

Bioorganic & Medicinal Chemistry

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Impact of refining on phytochemicals and anti-inflammatory activity of papaya (Carica papaya L.) seed oil in LPS-stimulated THP-1 cells

Peng,

Wang,

Farag

et al. 2024

Food Chemistry

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Structural modification based on the diclofenac scaffold: Achieving reduced colitis side effects through COX-2/NLRP3 selective inhibition

Cited by 4 publications

References 39 publications

Design, Synthesis and Biological Activities Evaluation of Novel Pterostilbene‐urea Derivatives as Potential Anti‐ inflammatory Agents

Design, Synthesis and Biological Activities Evaluation of Novel Pterostilbene‐urea Derivatives as Potential Anti‐ inflammatory Agents

Potential COX-2 inhibitors modulating NF-κB/MAPK signaling pathways: Design, synthesis and evaluation of anti-inflammatory activity of Pterostilbene-carboxylic acid derivatives with an oxime ether moiety

Impact of refining on phytochemicals and anti-inflammatory activity of papaya (Carica papaya L.) seed oil in LPS-stimulated THP-1 cells

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