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  • Effects of metformin on bile salt transport by monolayers of human intestinal Caco-2 cells.

Effects of metformin on bile salt transport by monolayers of human intestinal Caco-2 cells.

Diabetes, obesity & metabolism (2002-10-31)
D Carter, H C S Howlett, N F Wiernsperger, C Bailey
ABSTRACT

The antidiabetic biguanide metformin has been shown to increase faecal excretion of bile salts in type 2 diabetes. Cultured human intestinal Caco-2 cell monolayers provide a model of human enterocytes. These monolayers are used here to determine the effect of metformin on the secondary-active, sodium-linked transfer of 14C-glycocholate from the apical (brush border) to the basolateral (serosal) surface. During 24-h incubations, 10-2 mol/l metformin significantly reduced 14C-glycocholate transfer. This could not be attributed to alterations of monolayer integrity or Na+-K+ ATPase pump activity. For example, the secondary-active transport of glucose and proline was not interrupted, and the inhibitory effect of metformin on bile salt transport was additive to the inhibitory effect of ouabain. The results suggest that metformin can act directly on intestinal enterocytes to reduce the active transfer of bile salts by a mechanism that is independent of Na+-K+ ATPase activity.

MATERIALS
Product Number
Brand
Product Description

Supelco
Metformin hydrochloride, Pharmaceutical Secondary Standard; Certified Reference Material
Supelco
Metformin hydrochloride solution, 1.0 mg/mL in methanol (as free base), ampule of 1 mL, certified reference material, Cerilliant®
Sigma-Aldrich
1,1-Dimethylbiguanide hydrochloride, 97%
Metformin hydrochloride, European Pharmacopoeia (EP) Reference Standard