Document Detail

Characterization of the interaction between estrogen metabolites and taurocholate for uptake into isolated hepatocytes. Lack of correlation between cholestasis and inhibition of taurocholate uptake.
MedLine Citation:
PMID:  6727367     Owner:  NLM     Status:  MEDLINE    
The cholestasis induced by estrogen metabolites has been postulated to be due to an inhibition of bile acid transport. Therefore, the uptake of [3H]taurocholate (TC) into isolated hepatocytes was examined in the presence of known cholestatic steroid glucuronides. The cholestatic D-ring glucuronide conjugates of estradiol, estriol, ethynylestradiol and dihydrotestosterone did not inhibit the uptake of TC suggesting that these organic anions are transported by different carrier systems. Estrone sulfate inhibited TC uptake 65% but did not decrease bile flow following i.v. administration to the rat (22 mumol/kg), under conditions which the steroid glucuronide estradiol-17 beta-(beta-D-glucuronide) ( E217G ) decreased bile flow 100%. The hepatocytic uptake of [3H] E217G (100 microM) was inhibited by estriol-16 alpha-(beta-D-glucuronide) (200 microM, 40%) and estradiol-17 beta-3-(beta-D-glucuronide) (200 microM, 22%) as well as by the organic anions bromosulfophthalein (150 microM, 57%), dibromosulfophthalein (150 microM, 59%), indocyanine green (150 microM, 62%), rose bengal (150 microM, 56%) and bilirubin (50 microM, 40%). Thus, the bile acids and steroid glucuronides are transported into the hepatocyte by different carrier systems so that the cholestasis induced by the steroid D-ring glucuronides cannot be explained by an inhibition of bile acid uptake. Furthermore, the hepatocytic uptake of E217G occurs by a carrier system similar to that for the other steroid glucuronides and organic anions.
W J Brock; S Durham; M Vore
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Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Journal of steroid biochemistry     Volume:  20     ISSN:  0022-4731     ISO Abbreviation:  J. Steroid Biochem.     Publication Date:  1984 May 
Date Detail:
Created Date:  1984-06-28     Completed Date:  1984-06-28     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0260125     Medline TA:  J Steroid Biochem     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  1181-5     Citation Subset:  IM    
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MeSH Terms
Cholestasis / metabolism*
Dihydrotestosterone / analogs & derivatives,  pharmacology
Estradiol / analogs & derivatives,  metabolism
Estriol / analogs & derivatives,  pharmacology
Estrogens / metabolism*
Ethinyl Estradiol / analogs & derivatives,  pharmacology
Liver / metabolism*
Rats, Inbred Strains
Taurocholic Acid / metabolism*
Reg. No./Substance:
0/Estrogens; 0/ethinyl estradiol glucuronide; 1806-98-0/estradiol-17 beta-glucuronide; 28808-07-3/estriol glucuronide; 42037-24-1/dihydrotestosterone glucuronide; 50-27-1/Estriol; 50-28-2/Estradiol; 521-18-6/Dihydrotestosterone; 57-63-6/Ethinyl Estradiol; 81-24-3/Taurocholic Acid

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