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A pomegranate extract (PE) from the rind containing 90% ellagic acid was tested for its skin-whitening effect. PE showed inhibitory activity against mushroom tyrosinase in vitro, and the inhibition by the extract was comparable to that of arbutin, which is a known whitening agent. PE, when administered orally, also inhibited UV-induced skin pigmentation on the back of brownish guinea pigs. The intensity of the skin-whitening effect was similar between guinea pigs fed with PE and those fed with L-ascorbic acid. PE reduced the number of DOPA-positive melanocytes in the epidermis of UV-irradiated guinea pigs, but L-ascorbic acid did not. These results suggest that the skin-whitening effect of PE was probably due to inhibition of the proliferation of melanocytes and melanin synthesis by tyrosinase in melanocytes. PE, when taken orally, may be used as an effective whitening agent for the skin.

Metabolic conversion of flavonoids such as (+)-catechin and quercetin modifies the flavonoids' biological activity. Metabolites of flavonoids, rather than their intact forms, may contribute to the reported effects of flavonoids on reducing the risk of cardiovascular disease.

The effect of a single oral administration of proanthocyanidins, oligomeric and polymeric polyhydroxyflavan-3-ol units, on the antioxidative potential of blood plasma was studied in rats. Proanthocyanidin-rich extract from grape seeds was administered by intragastric intubation to fasted rats at 250 mg/kg of body weight. The plasma obtained from water- or proanthocyanidin-administered rats was oxidized by incubation with copper sulfate or 2, 2'-azobis(2-amidinopropane) dihydrochloride (AAPH) at 37 degrees C, and the formation of cholesteryl ester hydroperoxides (CE-OOH) was followed. The plasma obtained from proanthocyanidin-administered rats was significantly more resistant against both copper ion-induced and AAPH-induced formation of CE-OOH than that from control rats. The lag phase in the copper ion-induced oxidation of rat plasma was remarkably increased at 15 min after administration of proanthocyanidins and reached a maximum level at 30 min. When the plasma from proanthocyanidin-administered rat was hydrolyzed by sulfatase and beta-glucuronidase following analysis by high-performance liquid chromatography with electrochemical detection, metabolites of proanthocyanidins occurred in rat plasma at 15 min after administration, three peaks of which were identified as gallic acid, (+)-catechin, and (-)-epicatechin. These results suggest that the intake of proanthocyanidins, the major polyphenols in red wine, increases the resistance of blood plasma against oxidative stress and may contribute to physiological functions of plant food including wine through their in vivo antioxidative ability.

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SummaryWe performed a double-blind, placebo-controlled trial to clinically evaluate the protective and ameliorative effects of ellagic acid-rich pomegranate extract on pigmentation in the skin after ultraviolet ray (UV) irradiation, using female subjects in their 20s to 40s. Thirteen healthy volunteers per group were randomly assigned to three groups; namely, high dose (200 mg/d ellagic acid), low dose (100 mg/d ellagic acid) and control (0 mg/d ellagic acid: placebo). Each group received the respective test foods for 4 wk. Each subject received a 1.5 MED (minimum erythema dose) of UV irradiation on an inside region of the right upper arm, based on the MED value measured on the previous day. Luminance (L), melanin and erythema values were measured before the start of the test food intake, and after 1, 2, 3 and 4 wk following the start of the test food intake. Further, questionnaires were conducted regarding the condition of the skin before the start of the test food intake and at the termination of the test food intake. As a result, decreasing rates of L values from the baseline in the low-and high-dose groups were inhibited by 1.35% and 1.73% respectively, as compared to the control group. Further, a stratified analysis using subjects with a slight sunburn revealed an inhibited decrease of L values compared with the control group at 1, 2 ( p Ͻ 0.01, respectively) and 4 wk ( p Ͻ 0.05) after the start of the test food intake in the low-dose group, and at 2 and 3 wk ( p Ͻ 0.05) in the high-dose group. Furthermore, the results of questionnaires showed ameliorating tendencies due to the test food, in some items such as "brightness of the face" and "stains and freckles." Based on the above-mentioned results, it is suggested that ellagic acid-rich pomegranate extract, ingested orally, has an inhibitory effect on a slight pigmentation in the human skin caused by UV irradiation.