Document Detail


Inhibition of Na+-taurocholate Co-transporting polypeptide-mediated bile acid transport by cholestatic sulfated progesterone metabolites.
MedLine Citation:
PMID:  20177056     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Sulfated progesterone metabolite (P4-S) levels are raised in normal pregnancy and elevated further in intrahepatic cholestasis of pregnancy (ICP), a bile acid-liver disorder of pregnancy. ICP can be complicated by preterm labor and intrauterine death. The impact of P4-S on bile acid uptake was studied using two experimental models of hepatic uptake of bile acids, namely cultured primary human hepatocytes (PHH) and Na(+)-taurocholate co-transporting polypeptide (NTCP)-expressing Xenopus laevis oocytes. Two P4-S compounds, allopregnanolone-sulfate (PM4-S) and epiallopregnanolone-sulfate (PM5-S), reduced [(3)H]taurocholate (TC) uptake in a dose-dependent manner in PHH, with both Na(+)-dependent and -independent bile acid uptake systems significantly inhibited. PM5-S-mediated inhibition of TC uptake could be reversed by increasing the TC concentration against a fixed PM5-S dose indicating competitive inhibition. Experiments using NTCP-expressing Xenopus oocytes confirmed that PM4-S/PM5-S are capable of competitively inhibiting NTCP-mediated uptake of [(3)H]TC. Total serum PM4-S + PM5-S levels were measured in non-pregnant and third trimester pregnant women using liquid chromatography-electrospray tandem mass spectrometry and were increased in pregnant women, at levels capable of inhibiting TC uptake. In conclusion, pregnancy levels of P4-S can inhibit Na(+)-dependent and -independent influx of taurocholate in PHH and cause competitive inhibition of NTCP-mediated uptake of taurocholate in Xenopus oocytes.
Authors:
Shadi Abu-Hayyeh; Pablo Martinez-Becerra; Siti H Sheikh Abdul Kadir; Clare Selden; Marta R Romero; Myrddin Rees; Hanns-Ulrich Marschall; Jose J G Marin; Catherine Williamson
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-02-20
Journal Detail:
Title:  The Journal of biological chemistry     Volume:  285     ISSN:  1083-351X     ISO Abbreviation:  J. Biol. Chem.     Publication Date:  2010 May 
Date Detail:
Created Date:  2010-05-24     Completed Date:  2010-06-17     Revised Date:  2011-07-28    
Medline Journal Info:
Nlm Unique ID:  2985121R     Medline TA:  J Biol Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  16504-12     Citation Subset:  IM    
Affiliation:
Institute for Reproductive and Developmental Biology, Imperial College London, London W12 0NN, United Kingdom.
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MeSH Terms
Descriptor/Qualifier:
Animals
Bile Acids and Salts / chemistry,  metabolism
Binding, Competitive
Cell Line, Tumor
Cholestasis
Cobalt / chemistry*
Dose-Response Relationship, Drug
Female
Hepatocytes / metabolism
Humans
Models, Biological
Oocytes / metabolism
Peptides / chemistry
Pregnancy
Progesterone / chemistry*
Sodium / chemistry,  pharmacology*
Steroids / metabolism
Taurocholic Acid / chemistry*
Xenopus laevis
Chemical
Reg. No./Substance:
0/Bile Acids and Salts; 0/Peptides; 0/Steroids; 57-83-0/Progesterone; 7440-23-5/Sodium; 7440-48-4/Cobalt; 81-24-3/Taurocholic Acid
Comments/Corrections

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