Cholestatic steroid hormones inhibit taurocholate uptake into isolated rat hepatocytes

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

doi:10.1016/0006-2952(77)90453-1

Cholestatic steroid hormones inhibit taurocholate uptake into isolated rat hepatocytes

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

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Abstract

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 K_i 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 language	English
Pages (from-to)	2433-2437
Number of pages	5
Journal	Biochemical Pharmacology
Volume	26
Issue number	24
DOIs	https://doi.org/10.1016/0006-2952(77)90453-1
State	Published - 15 Dec 1977
Externally published	Yes

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title = "Cholestatic steroid hormones inhibit taurocholate uptake into isolated rat hepatocytes",

abstract = "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.",

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T1 - Cholestatic steroid hormones inhibit taurocholate uptake into isolated rat hepatocytes

AU - Schwarz, Leslie R.

AU - Schwenk, Michael

AU - Pfaff, Erich

AU - Greim, Helmut

PY - 1977/12/15

Y1 - 1977/12/15

N2 - 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.

AB - 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.

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DO - 10.1016/0006-2952(77)90453-1

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JO - Biochemical Pharmacology

JF - Biochemical Pharmacology

IS - 24

ER -

Cholestatic steroid hormones inhibit taurocholate uptake into isolated rat hepatocytes

Abstract

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