Metabolic fate of luteolin and its functional activity at focal site

Abstract Luteolin has been shown to possess potent antioxidant and anti‐inflammatory/anti‐allergic activities. In order to evaluate a chemopreventive role of luteolin in inflammatory responses involved in the pathogenesis of atherosclerosis and cancer etc., the metabolic fate of luteolin in rats and humans was investigated by HPLC analysis, and its effect on cell surface expression of adhesion molecules in human umbilical vein endothelial cells(HUVECs) was examined by ELISA. Luteolin monoglucuronide, which was a main metabolite, and free luteolin were detected in rat plasma and human serum. Luteolin monoglucuronide was hydrolyzed to free luteolin by β‐glucuronidase released from neutrophils stimulated with Ionomycin and Cytocharasine B. Luteolin suppressed the TNF‐α induced ICAM‐1 expression significantly. Among nine flavonoids (40 μM) examined, chrysin, apigenine, quercetin and galangin also demonstrated suppressive effct on it. These results suggest the posssibility that deconjugation of luteolin monoglucuronide occurs and that free luteolin showed functional acyivities such as suppression of TNF‐α induced ICAM‐1 expression at inflammation site.