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

D Carter, HCS Howlett, NF Wiernsperger, C Bailey*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review


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/I metformin significantly reduced 14Cycocholate 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 activily.

Original languageEnglish
Pages (from-to)424-427
Number of pages4
JournalDiabetes, Obesity and Metabolism
Issue number6
Publication statusPublished - Nov 2002


  • bile salts
  • Caco-2 cells
  • glycocholate
  • human intestinal enterocytes
  • intestinal transport
  • metformin


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