Anti-Inflamatory Activities of Novel Chalcone Derivatives

Russian Journal of Bioorganic Chemistry(2024)

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摘要
Objective: Design and synthesis of two chalcone derivatives, evaluation of their anticancer and antiinflamatory activities. Methods: The ring-closure through an intramolecular Friedel-Crafts reaction followed by an alkaline-catalyzed Claisen-Schmidt condensation. MTT assay was conducted in anticancer activity. The chalcone derivatives tested for anti-inflammatory immunomodulatory potential by measuring pro-inflammatory cytokines production levels. Results and Discussion: Both compounds displayed anti-inflammatory effects on activated mammalian cells without being cytotoxic. Their low toxicity resulted in high IC50 values in glioblastoma cells, indicating they are safe anti-inflammatory agents, yet lack anti-cancer properties. Conclusions: Synthesized and characterized two chalcone derivatives that displayed comparable anti-inflammatory effects, reducing TNF, IL6, GMCSF, and IL12p40 levels without harming macrophages. Their high IC50 values in glioblastoma cells suggest low toxicity and highlight their potential as effective anti-inflammatory agents
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关键词
chalcone,anti-inflammatory activity,glioblastoma,cytotoxicty,inflammation,macrophage
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