Dehydrocholic (jersey-5-β-cholic acid) was synthesized from cholic acid, with 200 mg of the mixed carrier and administered intravenously to two patients with T tube designed sampling of the indwelling bile without interrupting the enterohepatic circulation -hépatique allows. More than 80% of the radioactivity excreted was infused in the form of glycine conjugated bile acids and taurine in bile quickly. Radioactive products were identified after partially or completely reduced hepatic derivatives dehydrocholic. Mass spectrometry and chromatography, the main metabolite (about 70%) is a bile acid monoketo dihydroxybenzyl (cholanic acid 3α, 7α-dihydroxy-12-keto-5β); a second metabolite (approximately 20%) is a monohydroxy-diketo acid (cholanic 3α-hydroxy-7,12-di-keto-5β); and about 10% of the radioactivity was as cholic acid. The reduction appears to have been sequentially (3 positions, the positions 7 and 12 position) and stereospecific (only α epimer was recovered).
Bile, as the ratio between the flow of bile acid excretion in the bile expressed was increased by dehydrocholic administration. It was hypothesized that ketone hydroxylated metabolites are hydrocholeretics. not significantly change after the administration of the proportion of cholesterol into bile acids, lecithin and dehydrocholic. In vitro studies have shown that keto-hydroxy metabolites cholate are dispersed lecithin bad compared; However, mixtures of cholate and either a dispersion metabolite has similar properties to those alone, provided that the ratio of cholate metabolites for each metabolite remained cholate below a characteristic value. The experiments reveal a new metabolic pathway in humans, provide further insight into the hydrocholeresis induced keto bile acids, and show the remarkable change of pharmacological and physical properties. Replacement of hydroxyl group by a keto substituent in the bile acid molecule
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