Polymethoxyflavone Apigenin-Trimethylether Suppresses LPS-Induced Inflammatory Response in Nontransformed Porcine

Orsolya Farkas1, Orsolya Palócz1, Erzsébet Pászti-Gere1

  • 1Department of Pharmacology and Toxicology, Faculty of Veterinary Science, Szent István University, István utca 2, Budapest 1078, Hungary.

Insights

Apigenin and its methylated form reduce inflammation in intestinal cells. The methylated analogue, apigenin-trimethylether, shows greater effectiveness in mitigating lipopolysaccharide-induced inflammation and reducing inflammatory markers.

Area of Science:

  • Cell Biology
  • Pharmacology
  • Immunology

Background:

  • Flavonoids, like apigenin, possess anti-inflammatory properties.
  • Intestinal inflammation, often triggered by lipopolysaccharide (LPS), impacts epithelial cell function.
  • Investigating novel anti-inflammatory compounds is crucial for gut health.

Purpose of the Study:

  • To evaluate the in vitro anti-inflammatory effects of apigenin and apigenin-trimethylether.
  • To determine if these flavonoids can attenuate LPS-induced inflammation in intestinal epithelial cells (IPEC-J2).
  • To compare the efficacy of apigenin and its methylated analogue in reducing inflammatory markers.

Main Methods:

  • Utilized IPEC-J2 cells to model intestinal inflammation.
  • Administered apigenin and apigenin-trimethylether to LPS-treated cells.
  • Measured mRNA levels of inflammatory markers: IL-6, IL-8, TNF-α, and COX-2.
  • Assessed extracellular hydrogen peroxide (H2O2) levels using the Amplex Red assay.

Main Results:

  • Both apigenin and apigenin-trimethylether significantly reduced IL-8 gene expression.
  • Apigenin-trimethylether effectively decreased TNF-α mRNA levels, unlike apigenin.
  • Both compounds significantly lowered COX-2 mRNA levels, with the methylated analogue showing greater efficacy.
  • Apigenin (25 μM) reduced IL-6 mRNA, while apigenin-trimethylether did not at this concentration.
  • Both flavonoids significantly reduced extracellular H2O2 levels.

Conclusions:

  • Apigenin-trimethylether demonstrates significant potential in preventing LPS-induced intestinal inflammation.
  • The methylated apigenin analogue may serve as a future therapeutic agent for inflammatory conditions.
  • Flavonoids, particularly methylated derivatives, warrant further investigation for their anti-inflammatory applications in the gut.

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