Dichloroacetic acid: Metabolism in cytosol

Lipscomb, JC; Mahle, DA; Brashear, WT; Barton, HA

HERO ID

630723

Reference Type

Journal Article

Year

1995

Language

English

PMID

8591719

HERO ID 630723
In Press No
Year 1995
Title Dichloroacetic acid: Metabolism in cytosol
Authors Lipscomb, JC; Mahle, DA; Brashear, WT; Barton, HA
Journal Drug Metabolism and Disposition
Volume 23
Issue 11
Page Numbers 1202-1205
Abstract Dichloroacetic acid (DCA) arises from the chlorination of drinking water and the metabolism of trichloroethylene (TRI) and is used therapeutically. The toxicity of TRI exposure is dependent on metabolism, and DCA has been proposed to be one contributor to this toxicity. Beyond the identification of some metabolites of DCA and some pharmacokinetic studies, little is known about the tissue distribution and enzymology of DCA metabolism. We present data that indicate that DCA degradation occurs primarily in the cytosol. Low molecular weight components of cytosol are required for the reaction, including nicotinamide cofactor and glutathione (GSH). GSH plays a role in the removal of DCA from cytosol, although not through transferase-mediated conjugation. In rat cytosol, the KM is approximately 0.3 mM, and the apparent Vmax approximates 12 nmoles/min/mg cytosolic protein. These results set DCA apart from other chlorinated compounds that are metabolized by the cytochrome P450 enzyme family
Pmid 8591719
Url http://dmd.aspetjournals.org/content/23/11/1202.abstract
Is Certified Translation No
Dupe Override No
Is Public Yes
Language Text English
Keyword Animals; Atmospheric Pressure; Chromatography, Affinity; Cytochrome P-450 Enzyme System; Cytosol; Dichloroacetate; Drinking; Enzymology; Family; Glutathione; Liver; Male; metabolism; Mice; Mice, Inbred Strains; Microsomes, Liver; Molecular Weight; Nad; Rats; Rats, Inbred F344; Research; Subcellular Fractions; Tissue Distribution; Toxicity; Toxicology; Trichloroethylene; Water
Is Qa No