PT  - JOURNAL ARTICLE
AU  - Kayoko Shimoi
AU  - Noriko Saka
AU  - Ryushi Nozawa
AU  - Motoyoshi Sato
AU  - Izumi Amano
AU  - Tsutomu Nakayama
AU  - Naohide Kinae
TI  - Deglucuronidation of a Flavonoid, Luteolin Monoglucuronide, during Inflammation
DP  - 2001 Dec 01
TA  - Drug Metabolism and Disposition
PG  - 1521--1524
VI  - 29
IP  - 12
4099  - http://dmd.aspetjournals.org/content/29/12/1521.short
4100  - http://dmd.aspetjournals.org/content/29/12/1521.full
SO  - Drug Metab Dispos2001 Dec 01; 29
AB  - 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). β-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. β-Glucuronidase activity in human serum from patients on hemodialysis increased significantly compared with that from healthy volunteers. The β-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 β-glucuronidase is released from stimulated neutrophils or certain injured cells and then deglucuronidation of flavonoids occurs. The American Society for Pharmacology and Experimental Therapeutics