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

Leláková V., Smejkal K., Jakubczyk K., Veselý O., Landa P., Václavík J., Bobáľ P., Pížová H., Temml V., Steinacher T., Schuster D., Granica S., Hanáková Z., Hošek J.
FOOD CHEMISTRY 285: 431–440, 2019

Keywords: Anti-inflammatory, Cyclooxygenase, Molecular docking simulations, Lipoxygenase, Macrophage,s NF-κB, Stilbenes
Abstract: 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 aktivity 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.
DOI: 10.1016/j.foodchem.2019.01.128
IEB authors: Přemysl Landa