The effect of bile acids on drug metabolism

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Abstract
The major primary and secondary bile acids, cholic acid, chenodeoxycholic acid, deoxycholic acid, and lithocholic acid, affect the metabolism of one or more of the common substrates used to study the activity of liver drug‐metabolizing enzymes. Included were the mixed function oxidases that metabolize aniline, benzo(a)pyrene, 7‐ethoxy‐coumarin, p‐nitroanisole, aminopyrine, and testosterone. The microsomal epoxide hydrase was stimulated by the bile acids with the exception of chenodeoxycholic acid which was markedly inhibitory. The soluble glutathione‐S‐transferase was inhibited by all four bile acids. The potency of the effects varied with the substrate or bile acid used. These results demonstrate that the presence of bile acids could affect the metabolism of endogenous substrates, carcinogens, and other xenobiotics.