INVESTIGATION OF OVERINTAKE AND DRUG INTERACTION OF FUNCTIONAL FOOD COMPONENTS

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Functional foods have been used as prevention of several diseases in worldwide. Although its health benefit is noteworthy, the risk assessment of functional foods cannot be disregarded. In this study, I investigated the basic bioavailability of dietary polyphenol and the interaction between food components and medicine.Cranberry, which is rich in polyphenols including anthocyanins and proanthocyanidins, has been demonstrated to have various effects beneficial to human health including prevention of urinary tract infection. The bioavailability of cranberry polyphenols is little known. Forty-four metabolites in human urine after ingestion of cranberry juice were identified by using LC-ESI-MS/MS. Among metabolites, O-methylated proanthocyanidin A-2 were characterized as a new metabolite.Hydrolyzable tannins including ellagitannins occur in foods such as berries and nuts. Various biological activities, including antioxidant, antiviral and antitumor activities, have been noted and reported … More for ellagitannins, but the absorption and metabolism of purified ellagitannins are poorly understood. I investigated the characterization of urinary and intestinal microbial metabolites in rats after the ingestion of ellagitannin, geraniin. Rat urine sample was separated by column chromatography and/or preparative HPLC, to give seven metabolites, M1-M7. The structures of these metabolites were determined basis on spectroscopic data and chemical evidence. These compounds except for Ml were characterized as ellagitannin metabolites for the first time. Furthermore, among four major metabolites (M1-M4) in urine, M2 showed an antioxidant activity comparable to intact geraniin and related polyphenols.Interactions between food components and drugs have recently come into focus of interest. The interactions often occur as a result of inhibiting or inducing of the metabolic enzymes, cytochrome P450 (CYP). It is well known that concomitant intake with grapefruit juice increases the concentration of calcium antagonists in human by suppression of CYP3A4 activation. Cranberry juice has been traditionally used for the prevention of urinary tract infection. However, potentiated effects of warfarin following consumption of cranberry juice have been reported. The reasons for the interaction are mainly unknown. I study the inhibitory effects of cranberry extracts and ingredients, and related polyphenols on CYP2C9 and CYP3A4. Consequently, the gut microbial metabolites such as phenolic acids showed no effect. A part of compounds of coumarins, fiavones and flavonols exhibited a strong inhibitory activity.These results suggested that a part of dietary polyphenols might have the potential to inhibit the metabolism of drugs, so that further study should be investigated to clarify the clinical relevance. Less