Cholestatic steroid hormones inhibit taurocholate uptake into isolated rat hepatocytes

Leslie R. Schwarz, Michael Schwenk, Erich Pfaff, Helmut Greim

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The effect of three cholestatic steroids (norethandrolone, 17-β-estradiol and progesterone) on hepatocellular uptake and secretion of taurocholate was studied in isolated rat liver cells. The steroids decreased the rate of taurocholate uptake. Norethandrolone inhibited uptake noncompetitively with a Ki of 18 μM, but had no effect on the activation energy of uptake. 17-β-estradiol and progesterone reduced taurocholate uptake by 50 per cent at concentrations between 40 μM and 50 μM. The secretion of taurocholate from taurocholate-loaded cells was slightly increased by all three steroids at concentrations below 100 μM. A 60 per cent inhibition of secretion was observed in the presence of 500μM norethandrolone. Interference of cholestatic steroids with hepatocellular bile acid uptake may be an important step in the pathogenesis of intrahepatic cholestasis.

Original languageEnglish
Pages (from-to)2433-2437
Number of pages5
JournalBiochemical Pharmacology
Issue number24
StatePublished - 15 Dec 1977
Externally publishedYes


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