Tomatoes are widely consumed, however, studies on tomato seeds are limited. In this study, we isolated 11 compounds including saponins and flavonol glycosides from tomato seeds and evaluated their effects on epidermal hydration. Among the isolated compounds, tomato seed saponins (10 µM) significantly increased the mRNA expression of proteins related to epidermal hydration, including filaggrin, involucrin, and enzymes for ceramide synthesis, by 1.32- to 1.91-fold compared with the control in HaCaT cells. Tomato seed saponins (10 µM) also decreased transepidermal water loss by 7 to 13 g/m2·h in the reconstructed human epidermal keratinization (RHEK) models. Quantitative analysis of the ceramide content in the stratum corneum (SC) revealed that lycoperoside H (1–10 µM) is a promising candidate to stimulate ceramide synthesis via the upregulation of ceramide synthase-3, glucosylceramide synthase, and β-glucocerebrosidase, which led to an increase in the total SC ceramides (approximately 1.5-fold) in concert with ceramide (NP) (approximately 2-fold) in the RHEK models. Evaluation of the anti-inflammatory and anti-allergic effects of lycoperoside H demonstrated that lycoperoside H is suggested to act as a partial agonist of the glucocorticoid receptor and exhibits anti-inflammatory effects (10 mg/kg in animal test). These findings indicate that lycoperoside H can improve epidermal dehydration and suppress inflammation by increasing SC ceramide and steroidal anti-inflammatory activity.

Tomato seeds contain steroidal saponins called lycoperosides. However, it currently remains unclear whether lycoperosides exert anti‐inflammatory or anti‐allergic effects. Therefore, we herein investigated the effects of tomato seed extract (TSE) and lycoperoside H (LH) in Interleukin (IL)‐33 transgenic mice. TSE (500 mg/kg) or LH (10 mg/kg) was orally administered once a day for 101 days and then evaluated mouse behavior, skin symptoms, and blood and skin inflammatory cytokines. TSE slightly suppressed scratching behavior, while TSE and LH both increased locomotive activity. LH also significantly suppressed inflammation scores in the limbs, and TSE and LH reduced transepidermal water loss. Epidermal hyperplasia and the accumulation of eosinophils and mast cells were decreased by TSE and LH. Skin Th2/Th1 cytokine ratio and serum IgE concentrations were significantly reduced by TSE and LH. The present results suggest that the oral administration of LH derived from tomato seeds effectively ameliorates the symptoms of atopic dermatitis. Practical applications It has been reported that tomato seeds contain steroidal saponins, lycoperosides, though the effects of lycoperosides on anti‐inflammatory or anti‐allergic have not yet been revealed. In this study, we demonstrated that the oral administration of lycoperoside H derived from tomato seeds suppressed atopic dermatitis symptoms in IL‐33 transgenic mice.

Ampelopsis grossedentata (AG) is an ancient medicinal plant that is mainly distributed and used in southwest China. It exerts therapeutic effects, such as antioxidant, anti-diabetic, and anti-inflammatory activities, reductions in blood pressure and cholesterol and hepatoprotective effects. Researchers in China recently reported the anti-obesity effects of AG extract in diet-induced obese mice and rats. To verify these findings, we herein investigated the effects of AG extract and its principal compound, ampelopsin, in high-fat diet (HFD)- and alcohol diet-fed mice, olive oil-loaded mice, and differentiated 3T3-L1 cells. The results obtained showed that AG extract and ampelopsin significantly suppressed increases in the weights of body, livers and abdominal fat and also up-regulated the expression of carnitine palmitoyltransferase 1A in HFD-fed mice. In olive oil-loaded mice, AG extract and ampelopsin significantly attenuated increases in serum triglyceride (TG) levels. In differentiated 3T3-L1 cells, AG extract and ampelopsin promoted TG decomposition, which appeared to be attributed to the expression of hormone-sensitive lipase. In alcohol diet-fed mice, AG extract and ampelopsin reduced serum levels of ethanol, glutamic oxaloacetic transaminase (GOT), and glutamic pyruvic transaminase (GPT) and liver TG. An examination of metabolic enzyme expression patterns revealed that AG extract and ampelopsin mainly enhanced the expression of aldehyde dehydrogenase and suppressed that of cytochrome P450, family 2, subfamily e1. In conclusion, AG extract and ampelopsin suppressed diet-induced intestinal fat accumulation and reduced the risk of fatty liver associated with HFD and alcohol consumption.

Maqui berries are wildly grown or cultivated in the Patagonian region in Chile. The berries contain large amounts of anthocyanins, especially delphinidin glycosides, which are strong anti-oxidants. We previously reported that standardized maqui berry extract, which contained lots of anthocyanins, has ameliorative effects against dry eyes and visible light-induced photoreceptor cell damage. However, the influence of maqui berry extract on the human skin has not been evaluated even though many skin troubles are related to active oxygen species. Therefore, we conducted a randomized double-blind placebo-controlled pilot study with Delphinol®, a maqui berry extract standardized for anthocyanins, especially delphinidins and cyanidins, in healthy Japanese female subjects. Capsules containing Delphinol® (60 mg) or placebo were orally administered to subjects aged 27 to 57 years old for eight weeks. Skin conditions [pigmentation, redness, skin tone, wrinkles, texture, oil content, water content, trans epidermal water loss (TEWL), collagen score, dermal thickness, and elasticity] were measured before and after intervention. In the Delphinol® group, the saturation significantly increased after eight weeks and reddish spots significantly decreased after four weeks of intake. The collagen score, which decreases with age, slightly increased with age by Delphi-nol® ingestion for eight weeks. Thus, the anthocyanin-standardized maqui berry extract Delphinol® increased skin brightness and collagen content, and improved facial skin redness. This study suggests that the daily oral intake of maqui berry extract can help maintain a healthy facial condition.

Glucosylceramides (GlcCer), which are present in many edible plants, suppress melanin production in mouse melanocytes. Rice GlcCer consist of multiple molecules that comprise different types of sphingoid bases as well as diverse lengths and stereotypes of free fatty acids. Adjacent to the GlcCer fraction, there are free ceramides (Cer) as minor constituents. However, the anti‐melanogenic activities of individual GlcCer and Cer remain unknown. Therefore, we herein isolated 13 GlcCer and elasticamide, a Cer [AP] from the gummy by‐products of rice bran oil, and examined their anti‐melanogenic activities. In theophylline‐induced melanogenesis in B16 melanoma cells, GlcCer [d18:2(4E,8Z)/18:0], GlcCer [d18:2(4E,8Z)/20:0], and elasticamide significantly suppressed melanin production with IC50 values of 6.6, 5.2, and 3.9 μM, respectively. Elasticamide, but not GlcCer [d18:2 (4E,8Z)/20:0], suppressed melanogenesis in human 3D‐cultured melanocytes and the expression of tyrosinase‐related protein 1 in normal human melanocytes. Based on these results, we conducted a clinical trial on the effects of rice ceramide extract (Oryza ceramide®), containing 1.2 mg/day of GlcCer and 56 μg/day of elasticamide, on UV‐B‐induced skin pigmentation. The ingestion of Oryza ceramide® for 8 weeks significantly suppressed the accumulation of melanin 7 days after UV irradiation (1288 and 1546 mJ/cm2·S). Rice‐derived GlcCer and elasticamide, which exhibited anti‐melanogenic activities, were suggested to contribute to the suppressive effects of Oryza ceramide® on UV‐induced skin pigmentation. Although the mechanisms underlying the anti‐melanogenic activities of GlcCer remain unclear, elasticamide was identified as a promising Cer that exhibits anti‐melanogenic activity. Practical applications The anti‐melanogenic activities of rice‐derived GlcCer and elasticamide currently remain unclear. We herein demonstrated the inhibitory effects of individual GlcCer and elasticamide on melanogenesis in melanoma cells, melanocytes, and human skin.

Moriche palm is consumed as both a fresh fruit and processed food in Peru and Brazil. Although its fruit contains phytoestrogens, the active compounds have not yet been identified. Therefore, we purified moriche palm extract (MPE) and identified compounds exhibiting estrogenic and antiandrogenic activities. Estrogenic activity was assessed by the estrogen-dependent growth of MCF-7 cells and increases in uterine weights in mice. Antiandrogenic activity was evaluated by 5α-reductase inhibitory activity and prostate-specific antigen (PSA) expression in LNCaP cells. In vivo antiestrogenic activity was also assessed based on testosterone-induced prostate growth in castrated mice. Four methoxyflavans were isolated from MPE and all, except for 7,4′-dihydroxy-5-methoxyflavan, promoted MCF-7 cell growth, indicating estrogenic activity. Uterine and ovary weights increased in mice orally administered MPE (400 mg/kg) for 2 weeks. Regarding antiandrogenic activity, among the four methoxyflavans isolated, 6,7,4'-trihydroxy-5-methoxyflavan (1 µg/ml) suppressed the mRNA and protein expression of PSA in LNCaP cells. Furthermore, prostate growth was suppressed in mice orally administered MPE (200 mg/kg) for 2 weeks. All methoxyflavans inhibited 5α-reductase activity with IC 50 less than 10 µg/ml. Collectively, the present results demonstrated that orally administered MPE exhibited estrogenic and antiandrogenic activities. Methoxyflavans, particularly 6,7,4′-trihydroxy-5-methoxyflavan, appear to be the active compounds for these activities. Practical applications The fruit of Mauritia flexuosa (moriche palm) has been used for beverages and processed foods. Although it is said to contain phytoestrogens, the active compounds have not yet been identified. In this study, we isolated and identified methoxyflavans exhibiting estrogenic and antiandrogenic activities. Among them, 6,7,4′-trihydroxy-5-methoxyflavan appeared to be the most effective compounds for these activities.

Ceramide (Cer) plays an important role in skin barrier functions in the stratum corneum (SC). The ingestion of food-derived glucosylceramides (GlcCer) attenuates transepidermal water loss (TEWL). However, the moisturizing effects of single molecules of GlcCer and Cer remain unclear. Therefore, we herein purified 13 GlcCer and 6 Cer, including elasticamide, which has the same structure as human Cer[AP], from rice and compared their epidermal moisturizing effects in a reconstructed human epidermal keratinization model. The results obtained showed that 10 µM of 5 GlcCer[d18:2] with a 4E,8Z sphingadienine and C18 to C26 fatty acids and 10 µg/mL of 3 Cer with C23 or C24 fatty acids significantly reduced TEWL. The moisturizing effects of these GlcCer were dependent on the length of fatty acids. Furthermore, 10 µg/mL of elasticamide increased the SC Cer contents by promoting the expression of GlcCer synthase. Electron microscopic observations revealed that 1 µM of GlcCer[d18:2(4E,8Z)/26:0] increased the number of keratohyalin granules and desmosomes. Immunostaining and Western blotting indicated that 1 µM of GlcCer[d18:2(4E,8Z)/26:0] up-regulated the expression of filaggrin and corneodesmosin, which contribute to epidermal hydration. This comparative study on epidermal moisturization by GlcCer and Cer isolated from rice revealed differences in their hydration mechanisms.