2. Academic Validation
  3. Anti-Inflammatory Activity and ROS Regulation Effect of Sinapaldehyde in LPS-Stimulated RAW 264.7 Macrophages

Anti-Inflammatory Activity and ROS Regulation Effect of Sinapaldehyde in LPS-Stimulated RAW 264.7 Macrophages

  • Molecules. 2020 Sep 7;25(18):4089. doi: 10.3390/molecules25184089.
Seung-Hwa Baek 1 2,  Tamina Park 1 3,  Myung-Gyun Kang 1,  Daeui Park 1 2 3
Affiliations

Affiliations

  • 1 Department of Predictive Toxicology, Korea Institute of Toxicology, Daejeon 34114, Korea.
  • 2 Center for Convergent Research of Emerging Virus Infection, Korea Research Institute of Chemical Technology, Daejeon 34114, Korea.
  • 3 Department of Human and Environmental Toxicology, University of Science and Technology, Daejeon 34113, Korea.
PMID: 32906766 DOI: 10.3390/molecules25184089
Abstract

We evaluated the anti-inflammatory effects of SNAH in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages by performing nitric oxide (NO) assays, cytokine enzyme-linked immunosorbent assays, Western blotting, and real-time reverse transcription-polymerase chain reaction analysis. SNAH inhibited the production of NO (nitric oxide), Reactive Oxygen Species (ROS), tumor necrosis factor (TNF)-α, and interleukin (IL)-6. Additionally, 100 μM SNAH significantly inhibited total NO and ROS inhibitory activity by 93% (p < 0.001) and 34% (p < 0.05), respectively. Protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) stimulated by LPS were also decreased by SNAH. Moreover, SNAH significantly (p < 0.001) downregulated the TNF-α, IL-6, and iNOS mRNA expression upon LPS stimulation. In addition, 3-100 µM SNAH was not cytotoxic. Docking simulations and enzyme inhibitory assays with COX-2 revealed binding scores of -6.4 kcal/mol (IC50 = 47.8 μM) with SNAH compared to -11.1 kcal/mol (IC50 = 0.45 μM) with celecoxib, a known selective COX-2 Inhibitor. Our results demonstrate that SNAH exerts anti-inflammatory effects via suppression of ROS and NO by COX-2 inhibition. Thus, SNAH may be useful as a pharmacological agent for treating inflammation-related diseases.

Keywords

anti-inflammatory effect; cytokine; docking simulation; nitric oxide; reactive oxygen species; sinapaldehyde.

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