Anti-Inflammatory Activity of Rugchalcone Derivative on Lipopolysaccharides-Stimulated RAW264.7 Cells

Huiwon No and Jin-Kyung Kim

Background and Objective: Rugchalcones are isolated from the flowers of Rosa rugose. The pharmacological activities of rugchalcones and their derivatives are rarely reported. In the present study, we investigated the ability of Rugchalcone Derivative 4 (RD4) to regulate the inflammatory response in the RAW264.7 murine macrophage cell line. Material and Methods: To determine the anti-inflammatory effects of RD4, the lipopolysaccharide (LPS)-induced synthesis of inflammatory mediators in RAW264.7 cells were measured by Enzyme-Linked Immunosorbent Assay (ELISA) and Quantitative Real-Time Polymerase Chain Reaction (qRT-PCR). The anti-inflammatory mechanism of RD4 was investigated via western blot analysis of the activation of Nuclear Factor (NF)-κB and expression of Heme Oxygenase (HO)-1. Results: RD4 inhibited not only the synthesis of Nitric Oxide (NO) but also the expression of inducible NO synthase by LPS in the RAW264.7 murine macrophage cell line. RD4 inhibited the release of pro-inflammatory cytokines induced by LPS in RAW264.7 cells, including Interleukin (IL)-1β, IL-6 and tumour necrosis factor-α. The underlying anti-inflammatory mechanism of RD4 was correlated with the down-regulation of NF-κB and induction of HO-1. Conclusion: The data collectively indicate that RD4 inhibited the synthesis of several inflammatory mediators via regulation of NF-κB and HO-1 and represents a potential treatment for various inflammatory diseases.

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