Journal of Lipid Research, Vol 26, 583-592, Copyright © 1985 by Lipid Research, Inc.
Excretion of cholate glucuronide
JM Little, MV Chari and R Lester
[3-3H]Cholic acid glucuronide [7 alpha,12 alpha-dihydroxy-3 alpha-O-
(beta-D-glucopyranosyluronate)-5 beta- cholan-24-oate] was synthesized and
administered to rats prepared with either an external biliary fistula or a
ligated bile duct. When bile fistula animals were given either microgram or
milligram amounts of the glucuronide, biliary secretion of label was rapid
and efficient: greater than 90% of the administered label was secreted
within 60 min and total recovery of label in bile was 98.6 +/- 1.2%.
Studies in which [14C]taurocholate was included in the dose indicated that
this bile acid was secreted into bile significantly more rapidly than was
the glucuronide. In animals with ligated bile ducts, urinary excretion was
the major route of elimination: after 20 hr, 83.4 +/- 9.3% of the
administered dose had been excreted in urine. Urinary excretion of cholate
glucuronide was significantly more rapid than that of taurocholate.
Gas-liquid chromatographic analysis of the methyl ester acetate derivatives
of labeled compounds isolated from bile and urine by chromatography
established that the bulk (greater than 70%) of the administered material
was secreted in bile or excreted in urine as the intact cholate
glucuronide. From these results, we conclude that the glucuronidation of
cholic acid produces a derivative which is rapidly and effectively cleared
from the circulation and excreted.
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