Polymethoxyflavone Apigenin-Trimethylether Suppresses LPS-Induced Inflammatory Response in Nontransformed Porcine Intestinal Cell Line IPEC-J2.

Orsolya Farkas,Erzsébet Pászti-Gere,Péter Gálfi,Orsolya Palócz

doi:10.1155/2015/673847

Orsolya Farkas, Erzsébet Pászti-Gere + Show 2 more

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https://doi.org/10.1155/2015/673847

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Abstract

The in vitro anti-inflammatory effect of apigenin and its trimethylated analogue (apigenin-trimethylether) has been investigated in order to evaluate whether these flavonoids could attenuate LPS-induced inflammation in IPEC-J2 non-transformed intestinal epithelial cells. Levels of IL-6, IL-8, TNF-α, and COX-2 mRNA were measured as a marker of inflammatory response. The extracellular H2O2 level in IPEC-J2 cells was also monitored by Amplex Red assay. Our data revealed that both compounds had significant lowering effect on the inflammatory response. Apigenin (at 25 μM) significantly decreased gene expression of IL-6 in LPS-treated cells, while apigenin-trimethylether in the same concentration did not influence IL-6 mRNA level. Both apigenin and apigenin-trimethylether reduced IL-8 gene expression significantly. TNF-α mRNA level was decreased by apigenin-trimethylether, which was not influenced by apigenin. Treatment with both flavonoids caused significant reduction in the mRNA level of COX-2, but the anti-inflammatory effect of the methylated analogue was more effective than the unmethylated one. Furthermore, both flavonoids reduced significantly the level of extracellular H2O2 compared to the control cells. In conclusion, the methylated apigenin analogue could avoid LPS-induced intestinal inflammation and it could be applied in the future as an effective anti-inflammatory compound.

Highlights

Flavonoids are naturally occurring polyphenolic compounds which are part of the regular human diet, because of their presence in vegetables, fruits, and beverages such as wine, coffee, and tea
The main aim of this study is to investigate the possible protective effects of methoxyflavones in intestinal epithelial cells under the condition of inflammation
NF-κB activation resulted in the expression of a wide range of genes, many of which are markedly upregulated in response to microbial infection and inflammation

Summary

Introduction

Flavonoids are naturally occurring polyphenolic compounds which are part of the regular human diet, because of their presence in vegetables, fruits, and beverages such as wine, coffee, and tea. Many of the positive biological actions of flavonoids have been assigned to their antioxidant properties. There is an emerging view that flavonoids and their in vivo metabolites do not act only as conventional hydrogen-donating antioxidants but could modulate protein kinase signalling pathways in cells, influencing transcription factor nuclear factor kappa B (NF-κB) [2]. Polymethoxylated flavones (PMFs) or polymethoxyflavones are flavones substituted with two or more methoxy groups. They are coming into center of interest more and more due to their documented wide spectrum of biological activity including anti-inflammatory, anticarcinogenic, and antiatherogenic properties [4,5,6,7]. A novel tangeretin derivative, 5-acetyl-6,7,8,4󸀠-tetramethylnortangeretin, inhibited MCF-7 breast cancer cell growth through both caspase-dependent intrinsic apoptosis and caspase-independent apoptosis pathways [10]

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