Anti-Inflamatory Activities of Novel Chalcone Derivatives

Yalçın E., Sevin S., Uyar R., Ayaz F.

Russian Journal of Bioorganic Chemistry, vol.50, no.2, pp.432-443, 2024 (SCI-Expanded) identifier

  • Publication Type: Article / Article
  • Volume: 50 Issue: 2
  • Publication Date: 2024
  • Doi Number: 10.1134/s1068162024030762
  • Journal Name: Russian Journal of Bioorganic Chemistry
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, BIOSIS, Biotechnology Research Abstracts, Chemical Abstracts Core
  • Page Numbers: pp.432-443
  • Keywords: anti-inflammatory activity, chalcone, cytotoxicty, glioblastoma, inflammation, macrophage
  • Ankara University Affiliated: Yes

Abstract

Abstract: 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