Competitive inhibition of intestinal bile salt absorption in the rat

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Abstract
Competitive inhibition of intestinal C14-labeled taurocholate and cholate absorption by slices of rat ileum was observed in the presence of low concentrations of other conjugated and unconjugated bile salts. The affinity of the dihydroxycholanic acid derivatives for this common transport site was greater than of the cholate derivatives. Changes in the amino acid side chain did not greatly influence inhibition. Higher concentrations of chenodeoxycholate and deoxycholate produced cellular damage and noncompetitive inhibition of cholate absorption. These data indicate that several mechanisms for inhibition of intestinal transport of bile salts exist. The carrier -dependent competitive inhibition demonstrated at low concentrations appears to be the most susceptible to alteration.

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