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). 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.
Footnotes
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This work was supported by Special Coordination Funds of the Ministry of Education, Culture, Sports, Science, and Technology, the Japanese Government, and a grant from The Danone Institute of Japan. We thank Oryza Oil and Fat Chemical Co., Ltd. for providing luteolin.
- Abbreviations used are::
- HPLC
- high-performance liquid chromatography
- LPS
- lipopolysaccharide
- Received March 12, 2001.
- Accepted August 20, 2001.
- The American Society for Pharmacology and Experimental Therapeutics
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