Role for PPARgamma in IL-2 inhibition in T cells by Echinacea-derived undeca-2E-ene-8,10-diynoic acid isobutylamide

Int Immunopharmacol. 2009 Oct;9(11):1260-4. doi: 10.1016/j.intimp.2009.08.009. Epub 2009 Aug 25.

Abstract

Certain fatty acid amides from Echinacea spp. have demonstrated moderate to high cannabinoid activity. As a result, CB2 activation is currently hypothesized to be the basis of activity for immunomodulation by Echinacea spp. PPARgamma, an orphan nuclear receptor and lipid sensor, is known to inhibit IL-2 production and be activated by fatty acid derivatives such as the endocannabinoids. In these investigations, we demonstrate that undeca-2E-ene-8,10-diynoic acid, an Echinacea angustifolia-derived alkylamide lacking affinity for the CB2 receptor, inhibits IL-2 secretion in Jurkat T cells through PPARgamma activity at low micromolar concentrations (330 ng/mL). The IL-2 inhibition is reversed by the addition of the selective PPARgamma antagonist T0070907. Additionally, we show that that undeca-2-ene-8,10-diynoic acid stimulates 3T3-L1 differentiation, a process dependent on PPARgamma activity. These experiments demonstrate that PPARgamma is involved in T cell IL-2 inhibition by undeca-2-ene-8,10-diynoic acid and suggest that cytokine modulation by the alkylamides is due to polyvalent activity.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • 3T3-L1 Cells
  • Animals
  • Benzamides / pharmacology
  • Cell Differentiation / drug effects
  • Cell Differentiation / physiology
  • Cell Survival / drug effects
  • Drug Interactions
  • Echinacea / metabolism
  • Humans
  • Interleukin-2 / antagonists & inhibitors*
  • Interleukin-2 / metabolism
  • Jurkat Cells
  • Mice
  • PPAR gamma / antagonists & inhibitors
  • PPAR gamma / physiology*
  • Polyunsaturated Alkamides / pharmacology*
  • Pyridines / pharmacology

Substances

  • Benzamides
  • Interleukin-2
  • PPAR gamma
  • Polyunsaturated Alkamides
  • Pyridines
  • T 0070907