The action of GLP-1 and exendins upon glucose transport in normal human adipocytes, and on kinase activity as compared to morbidly obese patients

Int J Mol Med. 2007 Jun;19(6):961-6.

Abstract

A role of GLP-1 (glucagon-like peptide-1) in the recovery of the metabolic conditions of morbidly obese patients after bariatric surgery has been proposed. Exendin 4 (Ex-4) and exendin 9 (Ex-9) both have GLP-1-like effects upon glucose metabolism in human myocytes. We investigated in normal human adipocytes the effect of GLP-1, Ex-4 and Ex-9, compared with insulin upon the activity of PI3K, PKB, MAPKs and p70s6 kinases, and the participation of these enzymes in their action upon 2-deoxy-D-glucose transport by using potential inhibitors. The study was extended to morbidly obese patients. In normal subjects, GLP-1, Ex-4 and insulin, but not Ex-9, increased glucose uptake. In addition, GLP-1 and Ex-4 stimulated PI3K and MAPKs, similar to insulin, but not PKB. Ex-9 only enhanced PI3K, while none affected p70s6k. Inhibition of both PI3K and MAPKs blocked the stimulatory action of GLP-1, Ex-4 and insulin upon glucose transport. In obese patients, basal PI3K, PKB and MAPK activity was, as a rule, lower than that in normal subjects, while cells maintained their normal incremental response to GLP-1, Ex-4 or insulin; Ex-9 induced a clear stimulation of p42 MAPK. In summary, in normal human adipocytes, GLP-1 and Ex-4 have a protein kinase-dependent increasing effect upon glucose transport, which is impaired in obese patients. The participation of GLP-1 in the normalization of the metabolic conditions of the obese may occur through its effects on lipid metabolism or through effects upon glucose transport and/or metabolism in the liver and muscle, which in human obesity remain to be investigated.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adipocytes / drug effects*
  • Adipocytes / metabolism
  • Adult
  • Biological Transport / drug effects
  • Cells, Cultured
  • Deoxyglucose / pharmacokinetics
  • Exenatide
  • Female
  • Glucagon-Like Peptide 1 / pharmacology*
  • Glucose / metabolism*
  • Humans
  • Male
  • Middle Aged
  • Obesity, Morbid / metabolism*
  • Obesity, Morbid / pathology
  • Peptide Fragments / pharmacology*
  • Peptides / pharmacology*
  • Phosphotransferases / metabolism*
  • Venoms / pharmacology*

Substances

  • Peptide Fragments
  • Peptides
  • Venoms
  • exendin (9-39)
  • Glucagon-Like Peptide 1
  • Deoxyglucose
  • Exenatide
  • Phosphotransferases
  • Glucose