Characterization of the Synergistic Effect between Ligands of Opioid and Free Fatty Acid Receptors in the Mouse Model of Colitis

Molecules. 2021 Nov 11;26(22):6827. doi: 10.3390/molecules26226827.

Abstract

Background: Recent studies suggest that lipids, including free fatty acids (FFAs), are necessary for proper μ opioid receptor (MOR) binding and that activation of opioid receptors (ORs) improves intestinal inflammation. The objective of the study was to investigate a possible interaction between the ORs and FFA receptors (FFARs) ligands in the colitis.

Methods: The potential synergistic effect of ORs and FFARs ligands was evaluated using mouse model of acute colitis induced by dextran sulfate sodium (DSS, 4%). Compounds were injected intraperitoneally (i.p.) once or twice daily at the doses of 0.01 or 0.02 mg/kg body weight (BW) (DAMGO-an MOR agonist), 0.3 mg/kg BW (DPDPE-a δ OR (DOR) agonist) and 1 mg/kg BW (naloxone-a non-selective OR antagonist, GLPG 0974-a FFAR2 antagonist, GSK 137647-a FFAR4 agonist and AH 7614-a FFAR4 antagonist) for 4 days.

Results: Myeloperoxidase (MPO) activity was significantly decreased after DAMGO (0.02 mg/kg BW) and GSK 137647 (1 mg/kg BW) administration and co-administration as compared to DSS group.

Conclusions: Treatment with ligands of ORs and FFARs may affect the immune cells in the inflammation; however, no significant influence on the severity of colitis and no synergistic effect were observed.

Keywords: DAMGO; colitis; free fatty acid receptors; lipids; opioid receptor.

MeSH terms

  • Aniline Compounds / administration & dosage
  • Animals
  • Butyrates / administration & dosage
  • Colitis / drug therapy*
  • Colitis / immunology
  • Colitis / metabolism*
  • Disease Models, Animal
  • Drug Synergism
  • Enkephalin, Ala(2)-MePhe(4)-Gly(5)- / administration & dosage
  • Enkephalin, D-Penicillamine (2,5)- / administration & dosage
  • Inflammation / drug therapy
  • Inflammation / metabolism
  • Ligands
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Naloxone / administration & dosage
  • Narcotic Antagonists / administration & dosage
  • Peroxidase / metabolism
  • Receptors, G-Protein-Coupled / agonists
  • Receptors, G-Protein-Coupled / antagonists & inhibitors
  • Receptors, G-Protein-Coupled / metabolism*
  • Receptors, Opioid / agonists
  • Receptors, Opioid / metabolism*
  • Receptors, Opioid, delta / agonists
  • Receptors, Opioid, delta / metabolism
  • Receptors, Opioid, mu / agonists
  • Receptors, Opioid, mu / metabolism
  • Sulfonamides / administration & dosage
  • Thiophenes / administration & dosage
  • Xanthenes / administration & dosage

Substances

  • 4-(((R)-1-(benzo(b)thiophene-3-carbonyl)-2-methyl-azetidine-2-carbonyl)-(3-chloro-benzyl)-amino)-butyric acid
  • AH7614
  • Aniline Compounds
  • Butyrates
  • FFAR4 protein, mouse
  • Ffar2 protein, mouse
  • GSK137647
  • Ligands
  • Narcotic Antagonists
  • Receptors, G-Protein-Coupled
  • Receptors, Opioid
  • Receptors, Opioid, delta
  • Receptors, Opioid, mu
  • Sulfonamides
  • Thiophenes
  • Xanthenes
  • Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
  • Naloxone
  • Enkephalin, D-Penicillamine (2,5)-
  • Peroxidase