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Deglucuronidation of a flavonoid, luteolin monoglucuronide, during inflammation.

Abstract
In this study, we investigated whether luteolin monoglucuronide was converted to free aglycone during inflammation using human neutrophils stimulated with ionomycin/cytochalasin B and rats treated with lipopolysaccharide (LPS). beta-Glucuronidase activity was assayed using 4-methylumbelliferyl-glucuronide and methanol extracts of rat plasma containing luteolin monoglucuronide. The released 4-methylumbelliferone, a fluorescent molecule, was quantified by fluorometry. Deglucuronidation of luteolin monoglucuronide was examined by high-performance liquid chromatography (HPLC) analysis. HPLC analyses showed that the supernatants obtained from neutrophils stimulated with ionomycin/cytochalasin B hydrolyzed luteolin monoglucuronide to free luteolin. beta-Glucuronidase activity in human serum from patients on hemodialysis increased significantly compared with that from healthy volunteers. The beta-glucuronidase activity in rat plasma increased after i.v. injection of LPS. The ratio of luteolin to luteolin monoglucuronide in plasma of LPS-treated rats also increased. These results suggest that during inflammation beta-glucuronidase is released from stimulated neutrophils or certain injured cells and then deglucuronidation of flavonoids occurs.
AuthorsK Shimoi, N Saka, R Nozawa, M Sato, I Amano, T Nakayama, N Kinae
JournalDrug metabolism and disposition: the biological fate of chemicals (Drug Metab Dispos) Vol. 29 Issue 12 Pg. 1521-4 (Dec 2001) ISSN: 0090-9556 [Print] United States
PMID11717168 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Expectorants
  • Flavonoids
  • Glucuronides
  • Ionophores
  • Lipopolysaccharides
  • Cytochalasin B
  • Ionomycin
  • Glucuronidase
  • Luteolin
Topics
  • Animals
  • Chromatography, High Pressure Liquid
  • Cytochalasin B (pharmacology)
  • Expectorants (metabolism)
  • Flavonoids (metabolism)
  • Glucuronidase (metabolism)
  • Glucuronides (metabolism)
  • Humans
  • In Vitro Techniques
  • Inflammation (metabolism)
  • Ionomycin (pharmacology)
  • Ionophores (pharmacology)
  • Lipopolysaccharides (pharmacology)
  • Luteolin
  • Neutrophils (drug effects, metabolism)
  • Rats
  • Rats, Sprague-Dawley

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