TABLE 2

Summary of the in vitro properties of different bile acids reported in the literature

Bile AcidSULT2A1 Vmax/Km (µl/min per mg)bBSEP Uptake (pmol/mg per 30 s)cMRP4 Uptake Vmax/Km (µL/min per mg)dNTCP (OATP) Cell Uptake (fmol/min)eFXR (PXR) (CAT Activity -Fold Increase)fHydrophobicity Indexg
LCA23.3<45a35 (15)
G-LCA22.5+1.05
T-LCA16.7+1.0
DCA0.6340 (3)+0.72
G-DCA0.1717+0.65
T-DCA0.14600+0.59
CDCA0.12<45120 (3)+0.59
G-CDCA0.16100016+0.51
T-CDCA0.0114002329 (0.9)+0.46
CA<0.014552 (0.3)5 (2)+0.13
G-CA<0.01100714 (0.1)+0.07
T-CA<0.014002030 (0.1)0
UDCA0.91<4510 (−)−0.31
G-UDCA1.0230010−0.43
T-UDCA0.964001740 (1.8)−0.47
  • CA, cholic acid; CDCA, chenodeoxycholic acid; DCA, deoxycholic acid; G-CA, glycocholic acid; G-CDCA, glycochenodeoxycholic acid; G-DCA, glycodeoxycholic acid; G-LCA, glycolithocholic acid; G-UDCA, glycoursodeoxycholic acid; LCA, lithocholic acid; T-CA, taurocholic acid; T-CDCA, taurochenodeoxycholic acid; T-DCA, taurodeoxycholic acid; T-LCA, taurolithocholic acid; T-UDCA, tauroursodeoxycholic acid; UDCA, ursodeoxycholic acid.

  • a No data reported.

  • b Huang et al., 2010 (authors reported kinetic parameters for the sulfation of each BA after incubation with recombinant human sulfotransferase 2A1, SULT2A1).

  • c Hayashi et al., 2005 [authors reported BA uptake rate by human bile salt export pump (BSEP) vesicles and vector control vesicles; data represent difference between the two].

  • d Rius et al., 2005 [authors reported kinetic parameters for BA uptake by human multidrug resistance-associated protein 4 (MRP4) vesicles].

  • e Meier et al., 1997 [authors reported BA uptake rate into oocytes containing human sodium-taurocholate cotransporting polypeptide (NTCP) or human organic anion transporting peptide (OATP)].

  • f Parks et al., 1999; Staudinger et al., 2001 [human farnesoid X receptor (FXR)- and human pregnane X receptor (PXR)-mediated increase in chloramphenicol acetyltransferase (CAT) activity in CV-1 cells].

  • g Heuman et al., 1989.