scholarly journals Bile Acid Transporters Are Expressed and Heterogeneously Distributed in Rat Bile Ducts

Gut and Liver ◽  
2019 ◽  
Vol 13 (5) ◽  
pp. 569-575 ◽  
Author(s):  
Zhu-lin Luo ◽  
Long Cheng ◽  
Tao Wang ◽  
Li-jun Tang ◽  
Fu-zhou Tian ◽  
...  
Keyword(s):  
Bile Acid ◽  
Bile Ducts ◽  
Bile Acid Transporters ◽  
Rat Bile

The Orphan Nuclear Receptor, shp, Mediates Bile Acid-Induced Inhibition of the Rat Bile Acid Transporter, ntcp

2001 ◽  
Vol 121 (1) ◽  
pp. 140-147 ◽  
Author(s):  
Lee A. Denson ◽  
Ekkehard Sturm ◽  
Wihelma Echevarria ◽  
Tracy L. Zimmerman ◽  
Makoto Makishima ◽  
...  
Keyword(s):  
Bile Acid ◽  
Nuclear Receptor ◽  
Orphan Nuclear Receptor ◽  
Bile Acid Transporter ◽  
Acid Transporter ◽  
Rat Bile

scholarly journals Mechanism of Substrate Binding and Lipid Modulation in Bile Acid Transporters

2021 ◽  
Vol 120 (3) ◽  
pp. 303a-304a
Author(s):  
Azaan Wilbon ◽  
Jiemin Shen ◽  
Pei Qiao ◽  
Zachary J. Knepp ◽  
Wonpil Im ◽  
...  
Keyword(s):  
Bile Acid ◽  
Substrate Binding ◽  
Bile Acid Transporters

Effects of Age and Sex on Rat Bile Acid Metabolism

1971 ◽  
Vol 138 (2) ◽  
pp. 645-650 ◽  
Author(s):  
W. T. Beher ◽  
K. K. Casazza ◽  
G. J. Lin
Keyword(s):  
Bile Acid ◽  
Acid Metabolism ◽  
Bile Acid Metabolism ◽  
Rat Bile ◽  
Age And Sex

Differential intestinal deconjugation of taurine and glycine bile acid N-acyl amidates in rats

1992 ◽  
Vol 262 (2) ◽  
pp. G351-G358
Author(s):  
R. Zhang ◽  
S. Barnes ◽  
R. B. Diasio
Keyword(s):  
High Performance Liquid Chromatography ◽  
Small Intestine ◽  
Liquid Chromatography ◽  
Bile Acid ◽  
Chenodeoxycholic Acid ◽  
High Performance ◽  
Biliary Fistula ◽  
The Difference ◽  
The Stability ◽  
Rat Bile

Mechanisms responsible for the difference in the relative amounts of taurine- and glycine-conjugated bile acid N-acyl amidates (Tau/Gly ratio) are not fully understood. In the present study, the stability of taurine- and glycine-conjugated bile acid N-acyl amidates during intestinal transit and absorption was examined to investigate the contribution of intestinal deconjugation to the Tau/Gly ratio in rat bile. Radiolabeled chenodeoxycholic acid (CDC) and its N-acyl amidates with glycine (CDC-Gly) or taurine (CDC-Tau) were introduced into the lumen of the upper small intestine in the biliary fistula rats, and radioactive metabolites in bile, blood, urine, and tissues were identified and quantitated by high-performance liquid chromatography. Results indicated that 1) extensive deconjugation of CDC-Gly occurs during intestinal absorption; 2) CDC-Tau is recovered in bile largely intact; and 3) newly synthesized CDC-Tau and CDC-Gly are formed in a ratio of less than 2:1 after administration of [14C]-CDC. In summary, the present study demonstrates that resistance of taurine-conjugated bile acid N-acyl amidates to hydrolysis in the intestine, rather than a difference in synthesis of taurine- and glycine-conjugated N-acyl amidates in liver, may account for the high Tau/Gly ratio in rat bile.

scholarly journals Evaluating Hepatobiliary Transport with 18F-Labeled Bile Acids: The Effect of Radiolabel Position and Bile Acid Structure on Radiosynthesis and In Vitro and In Vivo Performance

2018 ◽  
Vol 2018 ◽  
pp. 1-9 ◽  
Author(s):  
Stef De Lombaerde ◽  
Ken Kersemans ◽  
Sara Neyt ◽  
Jeroen Verhoeven ◽  
Christian Vanhove ◽  
...  
Keyword(s):  
Bile Acid ◽  
Bile Acids ◽  
Membrane Vesicles ◽  
Hepatic Uptake ◽  
Hepatobiliary Transport ◽  
Bile Acid Transporters ◽  
Significant Difference ◽  
The Impact

Introduction. An in vivo determination of bile acid hepatobiliary transport efficiency can be of use in liver disease and preclinical drug development. Given the increased interest in bile acid Positron Emission Tomography- (PET-) imaging, a further understanding of the impact of 18-fluorine substitution on bile acid handling in vitro and in vivo can be of significance. Methods. A number of bile acid analogues were conceived for nucleophilic substitution with [18F]fluoride: cholic acid analogues of which the 3-, 7-, or 12-OH function is substituted with a fluorine atom (3α-[18F]FCA; 7β-[18F]FCA; 12β-[18F]FCA); a glycocholic and chenodeoxycholic acid analogue, substituted on the 3-position (3β-[18F]FGCA and 3β-[18F]FCDCA, resp.). Uptake by the bile acid transporters NTCP and OATP1B1 was evaluated with competition assays in transfected CHO and HEK cell lines and efflux by BSEP in membrane vesicles. PET-scans with the tracers were performed in wild-type mice (n=3 per group): hepatobiliary transport was monitored and compared to a reference tracer, namely, 3β-[18F]FCA. Results. Compounds 3α-[18F]FCA, 3β-[18F]FGCA, and 3β-[18F]FCDCA were synthesized in moderate radiochemical yields (4–10% n.d.c.) and high radiochemical purity (>99%); 7β-[18F]FCA and 12β-[18F]FCA could not be synthesized and included further in this study. In vitro evaluation showed that 3α-FCA, 3β-FGCA, and 3β-FCDCA all had a low micromolar Ki-value for NTCP, OATP1B1, and BSEP. In vivo, 3α-[18F]FCA, 3β-[18F]FGCA, and 3β-[18F]FCDCA displayed hepatobiliary transport with varying efficiency. A slight yet significant difference in uptake and efflux rate was noticed between the 3α-[18F]FCA and 3β-[18F]FCA epimers. Conjugation of 3β-[18F]FCA with glycine had no significant effect in vivo. Compound 3β-[18F]FCDCA showed a significantly slower hepatic uptake and efflux towards gallbladder and intestines. Conclusion. A set of 18F labeled bile acids was synthesized that are substrates of the bile acid transporters in vitro and in vivo and can serve as PET-biomarkers for hepatobiliary transport of bile acids.

Bile Acid-Dependent Secretion of Alkaline Phosphatase in Rat Bile

Hepatology ◽  
2007 ◽  
Vol 2 (4) ◽  
pp. 433S-439S ◽  
Author(s):  
David E. Hatoff ◽  
William G. M. Hardison
Keyword(s):  
Alkaline Phosphatase ◽  
Bile Acid ◽  
Rat Bile

Effects of Cys Mutation on Taurocholic Acid Transport by Mouse Ileal and Hepatic Sodium-dependent Bile Acid Transporters

2002 ◽  
Vol 66 (2) ◽  
pp. 467-470 ◽  
Author(s):  
Tohru SAEKI ◽  
Toshinori KURODA ◽  
Makiko MATSUMOTO ◽  
Ryuhei KANAMOTO ◽  
Kimikazu IWAMI
Keyword(s):  
Bile Acid ◽  
Taurocholic Acid ◽  
Acid Transport ◽  
Bile Acid Transporters ◽  
Sodium Dependent

Synthesis and biological evaluation of novel steroidal pyrazoles as substrates for bile acid transporters

2005 ◽  
Vol 15 (1) ◽  
pp. 85-87 ◽  
Author(s):  
Laxminarayan Bhat ◽  
Bernd Jandeleit ◽  
Tracy M. Dias ◽  
Tristen L. Moors ◽  
Mark A. Gallop
Keyword(s):  
Bile Acid ◽  
Biological Evaluation ◽  
Bile Acid Transporters ◽  
Synthesis And Biological Evaluation
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