NDLI: Identification of Human UDP-Glucuronosyltransferase Responsible for the Glucuronidation of Niflumic Acid in Human Liver

Content Provider	Springer Nature Link
Author	Ma, Yuji Usui, Takashi Kamimura, Hidetaka
Copyright Year	2006
Abstract	To assess the uridine diphosphate (UDP)-glucuronosyltransferase (UGT) isozymes involved in the glucuronidation of niflumic acid in human liver.The glucuronidation activity of niflumic acid was determined in liver microsomes and recombinant UGT isozymes by incubation of niflumic acid with UDP-glucuronic acid (UDPGA).Incubation of niflumic acid with liver microsomes and UDPGA produced one peak, which was identified as a glucuronide from mass spectrometric analysis. A study involving a panel of recombinant human UGT isozymes showed that glucuronidation activity was highest in UGT1A1 among the isozymes investigated. The glucuronidation in human liver microsomes (HLMs) followed Michaelis-Menten kinetics with a K$_{m}$ value of 16 μM, which is similar to that found with recombinant UGT1A1. The glucuronidation activity of niflumic acid in microsomes from eight human livers significantly correlated with UGT1A1-catalyzed estradiol 3β-glucuronidation activity (r=0.78, p<0.05). β-Estradiol inhibited niflumic acid glucuronidation with an IC$_{50}$ of 25 μM in HLMs, comparable to that for UGT1A1.These findings indicate that UGT1A1 is the main isozyme involved in the glucuronidation of niflumic acid in the human liver.
Starting Page	1502
Ending Page	1508
Page Count	7
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	23
Issue Number	7
e-ISSN	1573904X
Language	English
Publisher	Springer-Verlag
Publisher Date	2006-06-21
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	glucuronidation niflumic acid NSAID UGT1A1 Pharmacology/Toxicology Pharmacy Biochemistry Medical Law Biomedical Engineering
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science

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