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Effects of metformin on bile salt transport by monolayers of human intestinal Caco‐2 cells
Author(s) -
Carter D.,
Howlett H. C. S.,
Wiernsperger N. F.,
Bailey C.
Publication year - 2002
Publication title -
diabetes, obesity and metabolism
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.445
H-Index - 128
eISSN - 1463-1326
pISSN - 1462-8902
DOI - 10.1046/j.1463-1326.2002.00223.x
Subject(s) - biguanide , metformin , chemistry , ouabain , monolayer , brush border , caco 2 , medicine , endocrinology , small intestine , sodium , biochemistry , diabetes mellitus , cell , biology , membrane , vesicle , organic chemistry
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 14 C‐glycocholate from the apical (brush border) to the basolateral (serosal) surface. During 24‐h incubations, 10 −2 mol/l metformin significantly reduced 14 C‐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.