Parallel in vitro and in silico investigations into anti-inflammatory effects of non-prenylated stilbenoids

0502554 - ÚEB 2019 RIV NL eng J - Journal Article
Leláková, V. - Šmejkal, K. - Jakubczyk, Karolína - Veselý, Ondřej - Landa, Přemysl - Václavík, J. - Bobáľ, P. - Pížová, H. - Temml, V. - Steinacher, T. - Schuster, D. - Granica, S. - Hanáková, Z. - Hošek, J.
Parallel in vitro and in silico investigations into anti-inflammatory effects of non-prenylated stilbenoids.
Food Chemistry. Roč. 285, JUL 1 (2019), s. 431-440. ISSN 0308-8146. E-ISSN 1873-7072
R&D Projects: GA ČR(CZ) GA16-07193S
Institutional support: RVO:61389030
Keywords : Anti-inflammatory * Cyclooxygenase * Lipoxygenase * Macrophages * Molecular docking simulations * NF-κB * Stilbenes
OECD category: Biochemical research methods
Impact factor: 6.306, year: 2019

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.
Permanent Link: http://hdl.handle.net/11104/0294459