Impact of a glycogen phosphorylase inhibitor and metformin on basal and glucagon-stimulated hepatic glucose flux in conscious dogs

J Pharmacol Exp Ther. 2011 Jun;337(3):610-20. doi: 10.1124/jpet.110.177899. Epub 2011 Mar 1.

Abstract

The effects of a glycogen phosphorylase inhibitor (GPI) and metformin (MT) on hepatic glucose fluxes (μmol · kg(-1) · min(-1)) in the presence of basal and 4-fold basal levels of plasma glucagon were investigated in 18-h fasted conscious dogs. Compared with the vehicle treatment, GPI infusion suppressed net hepatic glucose output (NHGO) completely (-3.8 ± 1.3 versus 9.9 ± 2.8) despite increased glucose 6-phosphate (G-6-P) neogenesis from gluconeogenic precursors (8.1 ± 1.1 versus 5.5 ± 1.1). MT infusion did not alter those parameters. In response to a 4-fold rise in plasma glucagon levels, in the vehicle group, plasma glucose levels were increased 2-fold, and NHGO was increased (43.9 ± 5.7 at 10 min and 22.7 ± 3.4 at steady state) without altering G-6-P neogenesis (3.7 ± 1.5 and 5.5 ± 0.5, respectively). In the GPI group, there was no increase in NHGO due to decreased glucose-6-phosphatase flux associated with reduced G-6-P concentration. A lower G-6-P concentration was the result of increased net glycogenesis without altering G-6-P neogenesis. In the MT group, the increment in NHGO (22.2 ± 4.4 at 10 min and 12.1 ± 3.6 at steady state) was approximately half of that of the vehicle group. The lesser NHGO was associated with reduced glucose-6-phosphatase flux but a rise in G-6-P concentration and only a small incorporation of plasma glucose into glycogen. In conclusion, the inhibition of glycogen phosphorylase a activity decreases basal and glucagon-induced NHGO via redirecting glucose 6-phosphate flux from glucose toward glycogen, and MT decreases glucagon-induced NHGO by inhibiting glucose-6-phosphatase flux and thereby reducing glycogen breakdown.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood Glucose / metabolism
  • Dogs
  • Enzyme Inhibitors / pharmacology*
  • Fasting
  • Fatty Acids, Nonesterified / blood
  • Fatty Acids, Nonesterified / metabolism
  • Female
  • Glucagon / blood
  • Glucagon / metabolism
  • Glucagon / pharmacology
  • Gluconeogenesis / drug effects
  • Gluconeogenesis / physiology
  • Glucose / metabolism*
  • Glucose-6-Phosphatase / drug effects
  • Glucose-6-Phosphatase / physiology
  • Glycerol / blood
  • Glycerol / metabolism
  • Glycogen Phosphorylase, Liver Form / antagonists & inhibitors*
  • Glycogen Phosphorylase, Liver Form / metabolism
  • Hematocrit
  • Hypoglycemic Agents / pharmacology*
  • Indoles / pharmacology
  • Insulin / blood
  • Insulin / metabolism
  • Lactic Acid / blood
  • Lactic Acid / metabolism
  • Liver / drug effects*
  • Liver / metabolism
  • Liver Glycogen / metabolism*
  • Male
  • Metformin / pharmacology*
  • Phenylbutyrates / pharmacology

Substances

  • 3-(5-chloroindole-2-carbonyl)amino-2-hydroxy-4-phenylbutyric acid N-methyl-N-methoxyamide
  • Blood Glucose
  • Enzyme Inhibitors
  • Fatty Acids, Nonesterified
  • Hypoglycemic Agents
  • Indoles
  • Insulin
  • Liver Glycogen
  • Phenylbutyrates
  • Lactic Acid
  • Glucagon
  • Metformin
  • Glycogen Phosphorylase, Liver Form
  • Glucose-6-Phosphatase
  • Glucose
  • Glycerol