Analgesic and anti-inflammatory effectiveness of sitagliptin and vildagliptin in mice

Regul Pept. 2014 Nov:194-195:23-9. doi: 10.1016/j.regpep.2014.09.006. Epub 2014 Sep 16.

Abstract

To validate the potential anti-inflammatory and analgesic role of sita- and vildagliptin, five different experimental models were used in mice: i) mustard oil-induced ear edema, ii) neutrophil accumulation, iii) mechanical and iv) thermal touch sensitivity in complete Freund's adjuvant-induced arthritis and v) capsaicin-induced plasma extravasation in the urinary bladder. For the complete examination period in i) the dose of 10mg sitagliptin as well as 1-10mg vildagliptin was found to significantly decrease ear edema as compared to positive control (p<0.05, n=8/group). All doses of sitagliptin provided an anti-inflammatory effect p<0.005 (n=10/group) in test ii) and an analgesic effect in iii) except 3mg. Vildagliptin was similarly effective in test ii) (p<0.005, n=10/group) as sitagliptin, but it failed to affect mechanical touch sensitivity. Unlike mechanical touch sensitivity, both gliptins could beneficially act on the thermal threshold (p<0.05, n=10/group). And only in tests v) could both gliptins reverse inflammation. Further studies are needed to support the suggestion that the utilization of these beneficial effects of gliptins may be considered in the treatment of Type 2 diabetic patients.

Keywords: Arthritis; Mechanical and thermal touch sensitivity; Mice; Mustard oil; Sitagliptin; Vildagliptin.

MeSH terms

  • Adamantane / analogs & derivatives*
  • Adamantane / pharmacology
  • Allyl Compounds
  • Analgesics / pharmacology*
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Arthritis / drug therapy*
  • Capsaicin
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Edema / chemically induced
  • Edema / drug therapy*
  • Freund's Adjuvant
  • Isothiocyanates
  • Male
  • Mice
  • Nitriles / pharmacology*
  • Pyrrolidines / pharmacology*
  • Sitagliptin Phosphate / pharmacology*
  • Temperature
  • Urinary Bladder / drug effects
  • Vildagliptin

Substances

  • Allyl Compounds
  • Analgesics
  • Anti-Inflammatory Agents, Non-Steroidal
  • Isothiocyanates
  • Nitriles
  • Pyrrolidines
  • Freund's Adjuvant
  • Vildagliptin
  • Adamantane
  • Capsaicin
  • Sitagliptin Phosphate