SummaryThe concentrations of metabolites in human plasma after ingestion of flavanone glycosides (FG) and their aglycones (FA) in lemon were examined. FG consisting abundantly of eriocitrin were prepared from lemon peel and FA consisting abundantly of eriodictyol were prepared from FG by treatment with -glucosidase. Eriodictyol, homoeriodictyol, and hesperetin in plasma up to 4 h after ingestion of FG with water or FA with water by subjects were not detected in plasma of non-enzyme treatment but in plasma after treatment with -glucronidase and sulfatase. Metabolites in plasma after ingestion of FG and FA in humans were shown to exist as the glucuro-and/or sulfo-conjugates of eriodictyol, homoeriodictyol, and hesperetin. After ingestion of FA, the concentration of metabolites in plasma exhibited a high maximum peak at 1 h. The AUC (area under the blood concentration time curve) level of metabolites of FA was higher than that of FG. FA were suggested to be absorbed faster and in higher amounts than FG. The AUC of metabolites in subject plasma after ingestion of FG with flavonoid-depleted lemon juice was shown to change to a low level in comparison with that of FG with water. The maximum concentration peak of metabolites in plasma was faster at 0.5 h than FA with water but the AUC level was similar to FA with water, when subjects ingested FA with vodka (40% ethanol). The absorption hour of FG and FA was shown to be affected by the co-existing solution. Key Words lemon flavonoid, eriocitrin, plasma, human, ingestion Epidemiological studies indicate a protective relationship between the consumption of citrus fruits or juice and the risk of ischemic stroke and lung cancer (1, 2). Some fundamental studies support a protective effect provided by flavonoid consumption in these diseases (3-6). Citrus fruits contain various kinds of flavonoids such as flavanone glycoside, flavone glycoside, and polymethoxyflavone (3, 4). Flavonoids in lemon fruit (Citrus limon BURM. f.) have been reported to be such flavanone glycosides as eriocitrin (eriodictyol 7-O--rutinoside) and hesperidin (hesperetin 7-O--rutinoside) and such flavone glycosides as diosmin (diosmetin 7-O--rutinoside) and 6,8 C-diglucosyldiosmetin (7-10). Eriocitrin has been reported to be the most abundant flavonoid in lemon fruit and to have the highest antioxidative activity of the flavonoids in citrus fruits in vitro (9,11). It was also shown to have a suppressive effect for oxidative stress in the liver of streptozotocin-induced diabetic rats (12) or exercise-induced rats (13).For the study of functional compounds such as flavonoids in foods, it is important to determine how the compounds in food are metabolized and absorbed in vivo and how the metabolites function in a living system. There have been several human studies that have investigated the metabolism and absorption of flavonoids (14), such as anthocyanin (15, 16), flavonol (17, 18), isoflavone (19), and flavanone (20-22). As for eriocitrin, it was reported for metabolites by human intestinal bacteri...