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

Farkas O, Palócz O, Pászti-Gere E, Gálfi P - Oxid Med Cell Longev (2015)

Bottom Line: 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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacology and Toxicology, Faculty of Veterinary Science, Szent István University, István utca 2, Budapest 1078, Hungary.

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.

No MeSH data available.


Related in: MedlinePlus

Structure of apigenin (3′,4′,5-trihydroxyflavone) (a) and apigenin-trimethylether (3′,4′,5-trimethoxyflavone) (b).
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fig1: Structure of apigenin (3′,4′,5-trihydroxyflavone) (a) and apigenin-trimethylether (3′,4′,5-trimethoxyflavone) (b).

Mentions: The main aim of this study is to investigate the possible protective effects of methoxyflavones in intestinal epithelial cells under the condition of inflammation. Apigenin (3′,4′,5-trihydroxyflavone, Figure 1(a)), a well-studied and abundant flavonoid, and their methylated analogue (3′,4′,5-trimethoxyflavone, Figure 1(b)) were chosen as test compounds in order to study the abovementioned subject. This is the first report, which describes the effect of apigenin in intestinal inflammation using nontransformed intestinal epithelial cell line. Moreover, comparison of the anti-inflammatory effect of an unmethylated flavonoid and its methylated analogue in a nontransformed intestinal cell model was also performed at first time.


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

Farkas O, Palócz O, Pászti-Gere E, Gálfi P - Oxid Med Cell Longev (2015)

Structure of apigenin (3′,4′,5-trihydroxyflavone) (a) and apigenin-trimethylether (3′,4′,5-trimethoxyflavone) (b).
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4477253&req=5

fig1: Structure of apigenin (3′,4′,5-trihydroxyflavone) (a) and apigenin-trimethylether (3′,4′,5-trimethoxyflavone) (b).
Mentions: The main aim of this study is to investigate the possible protective effects of methoxyflavones in intestinal epithelial cells under the condition of inflammation. Apigenin (3′,4′,5-trihydroxyflavone, Figure 1(a)), a well-studied and abundant flavonoid, and their methylated analogue (3′,4′,5-trimethoxyflavone, Figure 1(b)) were chosen as test compounds in order to study the abovementioned subject. This is the first report, which describes the effect of apigenin in intestinal inflammation using nontransformed intestinal epithelial cell line. Moreover, comparison of the anti-inflammatory effect of an unmethylated flavonoid and its methylated analogue in a nontransformed intestinal cell model was also performed at first time.

Bottom Line: 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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacology and Toxicology, Faculty of Veterinary Science, Szent István University, István utca 2, Budapest 1078, Hungary.

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.

No MeSH data available.


Related in: MedlinePlus