Document Detail

Disposition of the novel antitumour agent xanthenone-4-acetic acid in the mouse: identification of metabolites and routes of elimination.
MedLine Citation:
PMID:  7975728     Owner:  NLM     Status:  MEDLINE    
1. Xanthenone-4-acetic acid (XAA) is an experimental antitumour agent which resembles flavone-8-acetic acid in its induction of cytokine synthesis, nitric oxide production and tumour haemorrhagic necrosis. We have investigated the excretion and metabolic fate of XAA in the BDF1 mouse. 2. XAA was administered intravenously at the maximal tolerated dose (1090 mumol/kg). Urine, plasma and bile were collected and subjected to analysis by hplc. Urine samples demonstrated labile metabolites which released XAA following incubation with beta-glucuronidase/sulphatase or at pH 9.0. The structures of isolated XAA metabolites were characterized by ms or 1H-NMR spectra at 400 MHz. 3. The major metabolite pathway of XAA involves conjugation with glucuronic acid, since the resulting metabolite, XAA acyl glucuronide, accounts for 25% of the dose excreted in the urine. Other metabolite pathways include alpha-oxidation of the acetic acid side chain and aromatic hydroxylation of the xanthenone ring.
P Kestell; G W Rewcastle; B C Baguley
Related Documents :
12884358 - Detection of the non-steroidal anti-inflammatory drug niflumic acid in humans: a combin...
7363468 - Conditions affecting the colorimetry of orotic acid and orotidine in urine.
17653568 - Comparative evaluation of biomarkers of occupational exposure to toluene.
7059658 - The identification of (e)-2-methylglutaconic acid, a new isoleucine metabolite, in the ...
8739518 - Biochemical characterization of lipopolysaccharides extracted from a hydrophobic strain...
18572898 - A pulse radiolysis investigation of the reactions of tributyl phosphate with the radica...
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Xenobiotica; the fate of foreign compounds in biological systems     Volume:  24     ISSN:  0049-8254     ISO Abbreviation:  Xenobiotica     Publication Date:  1994 Jul 
Date Detail:
Created Date:  1994-12-08     Completed Date:  1994-12-08     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1306665     Medline TA:  Xenobiotica     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  635-47     Citation Subset:  IM    
Cancer Research Laboratory, University of Auckland School of Medicine, New Zealand.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Antineoplastic Agents / metabolism*,  pharmacokinetics*
Bile / metabolism
Biliary Tract / metabolism
Chromatography, High Pressure Liquid
Dose-Response Relationship, Drug
Glucuronidase / metabolism
Mice, Inbred Strains
Sulfatases / metabolism
Xanthenes / metabolism*,  pharmacokinetics*,  urine
Reg. No./Substance:
0/Antineoplastic Agents; 0/Xanthenes; 35614-21-2/xanthenone-4-acetic acid; EC 3.1.6.-/Sulfatases; EC

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

Previous Document:  Use of organotypical cultures of primary hepatocytes to analyse drug biotransformation in man and an...
Next Document:  Metabolism of xilobam in laboratory animals and man.