Stilbenoids represent a large group of bioactive compounds, which occur in food and medicinal plants. Twenty-five stilbenoids were screened in vitro for their ability to inhibit COX-1, COX-2 and 5-LOX. Piceatannol and pinostilbene showed activity comparable to the zileuton and ibuprofen, respectively. The anti-inflammatory potential of stilbenoids was further evaluated using THP-1 human monocytic leukemia cell line. Tests of the cytotoxicity on the THP-1 and HCT116 cell lines showed very low toxic effects. The tested stilbenoids were evaluated for their ability to attenuate the LPS-stimulated activation of NF-κB/AP-1. Most of the tested substances reduced the activity of NF-κB/AP-1 and later attenuated the expression of TNF-α. The effects of selected stilbenoids were further investigated on inflammatory signaling pathways. Non-prenylated stilbenoids regulated attenuation of NF-ĸB/AP-1 activity upstream by inhibiting the phosphorylation of MAPKs. A docking study used to in silico analyze the tested compounds confirmed their interaction with NF-ĸB, COX-2 and 5-LOX.

• Klíčová slova
• Anti-inflammatory, Cyclooxygenase, Lipoxygenase, Macrophages, Molecular docking simulations, NF-κB, Stilbenes,
• MeSH
• antiflogistika nesteroidní chemie   farmakologie   MeSH
• HCT116 buňky MeSH
• inhibitory cyklooxygenasy 2 chemie   farmakologie   MeSH
• inhibitory lipoxygenas chemie   farmakologie   MeSH
• lidé MeSH
• lipopolysacharidy farmakologie   MeSH
• makrofágy účinky léků   metabolismus   MeSH
• NF-kappa B metabolismus   MeSH
• preklinické hodnocení léčiv metody   MeSH
• prenylace MeSH
• signální transdukce účinky léků   MeSH
• simulace molekulového dockingu MeSH
• stilbeny chemie   farmakologie   MeSH
• TNF-alfa metabolismus   MeSH
• transkripční faktor AP-1 metabolismus   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• 3,3',4,5'-tetrahydroxystilbene MeSH Prohlížeč
• antiflogistika nesteroidní MeSH
• inhibitory cyklooxygenasy 2 MeSH
• inhibitory lipoxygenas MeSH
• lipopolysacharidy MeSH
• NF-kappa B MeSH
• pinostilbene MeSH Prohlížeč
• stilbeny MeSH
• TNF-alfa MeSH
• transkripční faktor AP-1 MeSH