Antioxidant and anti-adipogenic activities of the nuts of Castanopsis cuspidata var. thunbergii.

The antioxidant and anti-adipogenic activities of the water extract (WE) and methanol extract (ME) of the shell and kernel of Castanopsis cuspidata var. thunbergii (CCT) nuts were evaluated. The shell extracts showed higher DPPH and ABTS radical scavenging activities (RSAs) than did the kernel extracts. Furthermore, the RSA of the ME was higher than that of the WE, regardless of the part. The total phenolic contents (TPCs) of the ME of the shell and kernel were 71.38 and 10.56 mg gallic acid equivalent (GAE)/100 mg extract, respectively. The TPCs of the WE of the shell and kernel were 17.44 and 9.27 mg GAE/100 mg extract, respectively. The WE inhibited 3T3-L1 adipogenesis more effectively than did the ME, and the shell extracts suppressed 3T3-L1 adipogenesis more effectively than did the kernel extracts. These results suggest that CCT nut kernels (ME) and shells (WE) may be strategically used to enhance antioxidant or and anti-obesity materials.

Anti-Adipogenic Effects of Ethanol Extracts Prepared from Selected Medicinal Herbs in 3T3-L1 Cells.

Obesity is a major risk factor for various metabolic diseases such as cardiovascular disease, hypertension, and type 2 diabetes mellitus. In this study, we prepared ethanol extracts from Agastache rugosa (ARE), Chrysanthemum zawadskii (CZE), Mentha arvensis (MAE), Perilla frutescens (PFE), Leonurus sibiricus (LSE), Gardenia jasminoides (GJE), and Lycopus coreanus (LCE). The anti-oxidant and anti-adipogenic effects were evaluated. The IC50 values for ascorbic acid and LCE against 2,2-diphenyl-1-picrylhydrazyl radicals were 246.2 µg/mL and 166.2 µg/mL, respectively, followed by ARE (186.6 µg/mL), CZE (198.6 µg/mL), MAE (337.1 µg/mL), PFE (415.3 µg/mL), LSE (548.2 µg/mL), and GJE (626.3 µg/mL). In non-toxic concentration ranges, CZE had a strong inhibitory effect against 3T3-L1 adipogenes (84.5%) than those of the other extracts. Furthermore, the anti-adipogenic effect of CZE is largely limited in the early stage of adipogenesis, and we revealed that the inhibitory role of CZE in adipogenesis is required for the activation of Wnt signaling. Our results provide scientific evidence that the anti-adipogenic effect of CZE can be applied as an ingredient for the development of functional foods and nutri-cosmetics for obesity prevention.

Study of Antiobesity Effect through Inhibition of Pancreatic Lipase Activity of Diospyros kaki Fruit and Citrus unshiu Peel.

Pancreatic lipase is the enzyme responsible for digestion and absorption of triglycerides, being its inhibition one of the widest studied methods used to determine the potential activity of natural products to inhibit dietary fat absorption. Decrease of energy intake from dietary fat through inhibition of this enzyme may be an excellent strategy to prevent and treat obesity. The inhibitory activity on pancreatic lipase enzyme of Diospyros kaki fruit and Citrus unshiu peel mixture extract (PCM) was evaluated in vitro and its antiobesity effects were studied based on the serum lipid parameters analysis from high-fat diet- (HFD-) fed mice in vivo. PCM was orally administered at a dose of 50 and 200 mg/kg body weight for 6 weeks. In addition, the activity of pancreatic lipase was assessed using orlistat (positive control). PCM exhibited inhibitory effect on lipase activity with IC50 value of 507.01 µg/mL. Moreover, serum triacylglycerol, total cholesterol levels, and visceral fat weight were significantly reduced compared to HFD control mice in PCM 200 mg/kg-treated mice (p < 0.05). These results suggest that PCM administration may be a novel potential antiobesity agent for reduction of fat absorption via inhibition of pancreatic lipase.

Antioxidant and Anti-Inflammatory Effects of Rhei Rhizoma and Coptidis Rhizoma Mixture on Reflux Esophagitis in Rats.

The purpose of this study was to investigate the antioxidant and anti-inflammatory effects of the combined extract of Rhei rhizoma and Coptidis rhizoma (RC-mix) in experimental model of acute reflux esophagitis. The antioxidant activity was assessed by in vitro 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays. RC-mix was given at 100, 200, and 400 mg/kg body weight 2 h prior to induction of reflux esophagitis (RE). After 5 h, the effects of RC-mix treated rats were compared with those of normal and control rats. The representative flavonoid contents of RC-mix, such as sennoside A, epiberberine, coptisine, palmatine, and berberine, were detected using HPLC. The elevated esophageal mucosa damage was markedly ameliorated by RC-mix treatment in a dose-dependent manner. Furthermore, the administration of RC-mix reduced the increase of serum reactive oxygen species (ROS) and peroxynitrite (ONOO(-)). The improvement of superoxide dismutase (SOD) and heme oxygenase-1 (HO-1) levels were marked in the group given RC-mix. Moreover, the elevation of inflammatory mediators and cytokines by nuclear factor-kappa B (NF-κB) activation in control rats decreased by RC-mix pretreatment. These results indicate that RC-mix treatment reduces the pathological states of esophagitis via regulating NF-κB mediated inflammation related to oxidative stress.

Protective effect of Rhei Rhizoma on reflux esophagitis in rats via Nrf2-mediated inhibition of NF-κB signaling pathway.

BACKGROUND: Rhei Rhizoma has been widely used as a traditional herbal medicine to treat various inflammatory diseases. The present study was conducted to evaluate its anti-inflammatory activity against experimental reflux-induced esophagitis (RE) in SD rats. METHODS: Rhei Rhizoma was administered at 125 or 250 mg/kg body weight per day for 7 days prior to the induction of reflux esophagitis, and its effect was compared with RE control and normal rats. RESULTS: Rhei Rhizoma administration markedly ameliorated mucosal damage on histological evaluation. The elevated reactive oxygen species in the esophageal tissue of RE control rats decreased with the administration of Rhei Rhizoma. RE control rats exhibited the down-regulation of antioxidant-related proteins, such as nuclear factor-erythroid 2-related factor 2 (Nrf2) and heme oxygenase-1 (HO-1) expression levels, in the presence of esophagitis; however, the levels with Rhei Rhizoma treatment were significantly higher than those in RE control rats. Moreover, RE control rats exhibited the up-regulation of protein expressions related to oxidative stress in the presence of esophagitis, but Rhei Rhizoma administration significantly reduced the expression of inflammatory proteins through mitogen-activated protein kinase (MAPK)-related signaling pathways. The protein expressions of inflammatory mediators and cytokines by nuclear factor-kappa B (NF-κB) activation were modulated through blocking the phosphorylation of inhibitor of nuclear factor kappa B (IκB)α. CONCLUSION: Our findings support the therapeutic evidence for Rhei Rhizoma ameliorating the development of esophagitis via regulating inflammation through the activation of the antioxidant pathway.

Anti-oxidant and anti-adipogenic effects of acorn (Quercus acutissima CARR.) shell extracts via regulation of wnt signaling in 3T3-L1 cells.

Acorn (Quercus acutissima CARR.) is a nut from the Fagaceae family that has been used in traditional medicine for many years. However, shells from acorns are regarded as a by-product and are mostly discarded. Anti-adipogenic activities of acorn shells were investigated using 3T3-L1 cells and methanol shell extracts (AE-M). AE-M demonstrated Cu2+-chelation activities and anti-oxidant activities via reduction of oxidative stress levels induced using AAPH. Six days after adipocyte differentiation, 50 and 100 µg/mL AE-M completely suppressed 3T3-L1 adipogenesis and the anti-adipogenic effect was stronger than for the positive control 50 µM quercetin. Treatment with AE-M in 3T3-L1 cells reduced mRNA expression levels of adipogenic genes. AE-M-inhibition was found in pre-adipogenic, early, and intermediate stages of adipogenesis in 3T3-L1 cells. The Wnt/ß-catenin signaling pathway is required for AE-M-inhibition of 3T3-L1 adipogenesis.

Antioxidant and anti-adipogenic activities of chestnut (Castanea crenata) byproducts.

The antioxidant and anti-adipogenic activities of chestnut byproducts were evaluated. At 100 µg/mL, the methanol extract (ME) scavenged 34.2% of DPPH and 78.8% of ABTS radicals. The DPPH and ABTS radical scavenging activity of the water extract (WE) was found to be low (13.7 and 33.1%, respectively) compared with controls. WE and ME dose-dependently inhibited lipid accumulation of 3T3-L1 adipocytes. WE and ME at 100 µg/mL suppressed 3T3-L1 adipogenesis by 71.0 and 96.5%, respectively, when compared with mature adipocytes. The results indicated that WE and ME inhibited adipocyte differentiation by down-regulating the mRNA expression levels of CCAAT/enhancer binding protein (C/EBP)-ß, C/EBPα, and peroxisome proliferator-activated receptor (PPAR)-γ in 3T3-L1 cells. Our study also revealed that WE and ME inhibited pre- and early stage adipogenesis in 3T3-L1 cells. The results suggest that chestnut byproducts are a promising source of antioxidant and antiobesity molecules.

Antioxidant and anti-adipogenic activities of acorn shells.

Antioxidant and anti-adipogenic activities of water extract (WE) and methanol extract (ME) of acorn shells (AS), from Quercus acutissima Carruth. grown in Korea, were investigated. At a concentration of 50 µg/mL, the WE had a scavenging activity of 53.84% for the DPPH and 76.09% for the ABTS radical, while the ME had corresponding scavenging activities of 29.09 and 48.43%. Total phenolic contents of WE and ME were 375.96 and 288.01 mg gallic acid equivalents/g of extracts, respectively. Both extracts significantly inhibited 3T3-L1 adipogenesis in a dose-dependent manner, and concomitantly decreased the size and number of intracellular lipid droplets. Furthermore, the antiadipogenic activities of WE and ME are largely limited in the pre- and early stages of adipogenesis. The results suggest that AS may be a promising source of antioxidants and anti-obesity compounds.

Beneficial role and function of fisetin in skin health via regulation of the CCN2/TGF-ß signaling pathway.

Skin is composed of multiple layers, including the epidermis, dermis, and hypodermis. Although several biological activities of fisetin have been reported, beneficial effects and the functions of fisetin in skin remain unclear. B16F10 melanoma cells, human skin fibroblasts, and 3T3-L1 cells were used to examine the beneficial effects of fisetin in skin health. α-MSH- and IBMX-induced melanosis in B16F10 melanoma cells was inhibited by fisetin treatment, which also enhanced mRNA expression levels of skin fibril-related genes via the CCN2/TGF-ß signaling pathway. Decreased intracellular lipid accumulation via down-regulation of transcriptional factors through activation of the CCN2/TGF-ß signaling pathway was observed. A novel function of fisetin in skin health via down-regulation of melanosis and adipogenesis, and up-regulation of skin fibril-related genes was observed. Evidence for development of nutri-cosmetics for skin health is presented.

Perception of childhood obesity in mothers of preschool children.

OBJECTIVES: The purpose of this study was to identify the perception of childhood obesity in mothers of preschool children using Q methodology. METHODS: A total of 38 Q statements about childhood obesity were obtained from 41 participants. The QUANL PC program was used to analyze the results. RESULTS: There were three types of perception toward obesity in mothers of preschool children: the "authoritative discipline type," the "generous home meal focused type," and the "home meal based on household financial situation type." CONCLUSION: The perception of mothers toward childhood obesity can affect the extent of maternal interaction with children or meal preparation for the family. Based on these results, it is necessary to plan specific programs according to the types of maternal perception toward childhood obesity.

Anti-Oxidant and Anti-Adipogenic Effects of Ethanol Extracts from Wheat Germ and Wheat Germ Fermented with Aspergillus oryzae.

Most of the wheat germ in cereal grains is removed during the milling process. Various physiological effects have been reported for bioactive substances in wheat germ such as phenolic acids and flavonoids. In this study, the anti-oxidant and anti-adipogenic effects of ethanol extracts from wheat germ (WGE) and wheat germ fermented with Aspergillus oryzae (F-WGE) were investigated in HepG2 and 3T3-L1 cells. The anti-oxidant activity of F-WGE was demonstrated by a dose-dependent increase in the enhanced scavenging capacity of hydroxyl radicals and Cu(2+)-chelating activity compared to WGE. WGE and F-WGE treatment at doses between 10 and 400 µg/mL did not affect the viability of HepG2 and 3T3-L1 cells. Intracellular ROS levels from Cu(2+)-induced oxidative stress were significantly decreased by F-WGE treatment in HepG2 cells compared to WGE. Lipid accumulation was increased in 3T3-L1 adipocytes by 100 µM Fe(2+) treatment, but the accumulation was strongly inhibited by 100 µg/mL of WGE and F-WGE treatment. These results suggest that changes in bioactive substances during the fermentation of wheat germ can potentiate scavenging activities against transition metal-induced oxidative stress and lipid accumulation in 3T3-L1 adipocytes. Therefore, we propose that F-WGE is a novel food materials and provided scientific evidences for its efficacy in the development of functional foods.

Anti-aging Potential of Extracts Prepared from Fruits and Medicinal Herbs Cultivated in the Gyeongnam Area of Korea.

Many recent studies have focused on maintaining a healthy life by preventing and/or postponing the aging process. Numerous studies have reported that continuous exposure to reactive oxygen species can stimulate skin aging and that excessive accumulation of fat can cause an impaired skin barrier and tissue structure alterations. Thus, the maintenance of antioxidant homeostasis and the suppression of adipose accumulation are important strategies for skin anti-aging. Here, we prepared three types of extracts [whole juice, acetone-perchloric acid (PCA), and ethanol] from 20 fruits and medicinal herbs native to the Gyeongnam area of Korea. The total phenolic content of each extract was analyzed, and we observed higher total phenolic contents in the medicinal herbs. Consistent with this, the results of the oxygen radical absorbance activity capacity assay indicated that the in vitro antioxidant activities of the medicinal herb extracts were stronger than those of the fruit extracts. The fruits and medicinal herbs had strong effects on cell-based systems, including H2O2-induced oxidative stress in human keratinocytes and 3T3-L1 lipid accumulation. Nishimura Wase persimmon, Taishu persimmon, wrinkled giant hyssop, sweet wormwood, Chinese cedar, red perilla, tan shen, hiyodori-jogo, and cramp bark may be natural anti-aging materials with effective antioxidant and anti-adipogenic activities. Taken together, our findings may provide scientific evidence supporting the development of functional foods and nutraceuticals from fruits and medicinal herbs.

Selenate inhibits adipogenesis through induction of transforming growth factor-ß1 (TGF-ß1) signaling.

Selenium is essential for many aspects of human health. While selenium is known to protect against cancer and cardiovascular diseases, the role of selenium in adipose development is unknown. Here we show that selenate at non-toxic concentration exhibits an anti-adipogenic function in vitro and ex vivo. In addition, selenate induced a morphological change of these cells from fibroblast-like to spindle cell shape. However, other forms of selenium, including selenite and methylseleninic acid, showed either toxic or no effect on adipogenesis and morphology change of preadipocytes. The effects of selenate on adipogenesis and cell morphology change were blunted by the treatment with SB431542, a specific inhibitor of transforming growth factor-ß1 (TGF-ß1) receptor, neutralization TGF-ß1 by its antibody, and knockdown of TGF-ß1 in preadipocytes, suggesting a requirement of TGF-ß signaling for the anti-adipogenic function of selenate. Among tested forms of selenium, selenate appears to be an effective activator of TGF-ß1 expression in preadipocytes. These results indicate that selenate is a novel dietary micromineral that activates TGF-ß1 signaling in preadipocytes and modulates adipogenesis.

In vitro and intracellular antioxidant capacity of thymyl methyl ether as a major component in Blumea lanceolaria (Roxb.) Druce leaf oil.

Thymyl methyl ether is a major component of Blumea lanceolaria (Roxb.) Druce leaves. In this study, the antioxidant capacity of thymyl methyl ether and its better known hydroxylated form thymol was examined using oxygen radical absorption capacity and intracellular antioxidant capacity assays. Thymol displayed stronger peroxyl radical and hydroxyl radical-scavenging capacity, as well as reducing capacity than those of thymyl methyl ether, which can be explained by its hydrogen or electron donating capacity. However, thymyl methyl ether exhibited potent protection against peroxyl radical and Cu(2+)-induced oxidative stress when compared to thymol in the intracellular antioxidant capacity and lipid peroxidation assays using HepG2 cells. These results illustrate the higher cell membrane permeability of thymyl methyl ether to thymol and its transformation to thymol, which results in potent intracellular antioxidant capacity contributing to protection against lipid peroxidation.

Mulberry leaf extract reduces postprandial hyperglycemia with few side effects by inhibiting α-glucosidase in normal rats.

Mulberry (Morus alba L.) leaf extract (MLE) was investigated as a potent plant-derived α-glucosidase inhibitor with low α-amylase inhibitory activity. MLE was prepared by heating in an autoclave at 121 °C for 15 minutes, and its in vitro and in vivo antihyperglycemic activities were investigated. The adverse side effects of MLE were analyzed by measuring the weight and volume of the cecum, stool color, starch content in the cecum, and the integrity of intestinal transporting capacity. The in vitro inhibitory activity of MLE on intestinal α-glucosidase was potent and that on intestinal α-amylase was very weak compared with acarbose. Sugar loading tests with starch, maltose, and sucrose showed that MLE may reduce postprandial increases in blood glucose by acting as an intestinal α-glucosidase inhibitor. Feeding tests suggested that MLE may exhibit fewer adverse side effects than other α-glucosidase inhibitors, such as abdominal flatulence and meteorism, which are attributed to the impaired digestion of starch by strong inhibition of intestinal α-amylase. These results suggest that MLE could be used in the development of pharmaceutical foods to control the blood glucose levels of diabetic patients by inhibiting intestinal α-glucosidase with reduced side effects.

Protective mechanism of quercetin and rutin on 2,2'-azobis(2-amidinopropane)dihydrochloride or Cu2+-induced oxidative stress in HepG2 cells.

Protective effects of quercetin and rutin against oxidative stress were evaluated using in vitro and intracellular antioxidant assay. Quercetin showed higher peroxyl and hydroxyl radical-scavenging activity in a dose-dependent manner than did rutin in oxygen-radical absorbance capacity (ORAC). At 10 and 100 µM, quercetin had higher metal-chelating activity than rutin carrying rutinose at position C-3 and was also more efficient than rutin in reducing intracellular oxidative stress caused by peroxyl radicals and Cu(2+). The protective activities of 10 and 100 µM quercetin against Cu(2+)-induced intracellular oxidation were 13.8% and 44.8%, respectively. Rutin showed no protective activity against Cu(2+)-induced oxidative stress. Quercetin showed significantly lower intracellular Cu(2+)-chelating activity than did 1,10-phenanthroline but offered greater protection from Cu(2+)-induced oxidative stress. Thus, quercetin may diffuse through the cell membrane more efficiently than rutin because quercetin does not carry rutinose, is hydrophilic, and reduces Cu(2+)-induced oxidative stress by scavenging radicals instead of chelating with metal ions.

Flavonol content in the water extract of the mulberry (Morus alba L.) leaf and their antioxidant capacities.

UNLABELLED: The biological activities of the mulberry (Morus alba L.) leaf have been attributed to its flavonoid content. The water extract of the mulberry leaf (WEML) was prepared by autoclaving at 121 °C for 15 min, and the flavonol content of the WEML was determined by HPLC The WEML contained 4 flavonols in the following order: quercetin-3-ß-D-glucose (QT-G) > quercetin-3-O-glucose-6″-acetate (QT-GA) > rutin (RT) > quercetin (QT). In the oxygen radical absorbance capacity (ORAC) assay, QT had the highest peroxyl radical-scavenging capacity and a similar hydroxyl radical-scavenging capacity as its glycosides (QT-G, QT-GA, and RT). QT exhibited a stronger cellular antioxidant capacity (CAC) against 2,2'-Azobis(2-amidinopropane) dihydrochloride (AAPH)- and Cu²âº-induced oxidative stress in HepG2 cells compared to its glycosides, indicating that the intracellular antioxidant capacity of QT and its glycosides may depend upon both the permeability across the cell membrane and the peroxyl or hydroxyl radical-scavenging capacity. PRACTICAL APPLICATION: The information presented might be used for developing mulberry leaf-based functional foods.

Heat processing decreases Amadori products and increases total phenolic content and antioxidant activity of Korean red ginseng.

The functional properties of Korean red ginseng (KRG) are known to be dependent upon the extent of heat processing. We demonstrated that repeated heat processing in the preparation of KRG decreased its arginyl-fructosyl-glucose (AFG) content and metal chelating capacity. On the other hand, the total phenolic compound content, in vitro peroxyl radical scavenging ability, and cellular peroxyl and hydroxyl radical scavenging ability increased with repeated heat processing. The peroxyl radical scavenging ability of KRG may be due to the total phenolic compound content. The hydroxyl radical scavenging ability of KRG seems to result mainly from the chelating ability of Amadori compounds such as arginyl-fructose and AFG. The protective ability of KRG against Cu²(+)-induced oxidative stress in hepatoma HepG2 cells may be due to permeability into the cell membrane rather than antioxidant activity. These results can be used to predict the physiological functions of KRG in in vivo models.

Two new C-glucosyl benzoic acids and flavonoids from Mallotus nanus and their antioxidant activity.

Two new 2-C-beta-D-glucopyranosyl benzoic acid derivatives named mallonanosides A (1) and B (2) were isolated from the methanolic extract of the leaves of Mallotus nanus along with five known flavonoids, kaempferin (3), juglanin (4), quercitrin (5), myricitrin (6), and rhoifolin (7). Their structures were established on the basis of spectral and chemical evidence. Their antioxidant activities were shown to depend on the number of hydroxyl groups, and the location and species of sugar moiety.

Protective mechanism of quercetin and rutin using glutathione metabolism on HO-induced oxidative stress in HepG2 cells.

The levels of cellular glutathione (GSH) and reactive oxygen species (ROS) simultaneously determined by fluorometric measurement, may provide important information on pro-oxidative and antioxidative balance. The dual effect of quercetin antioxidant and pro-oxidant activity was proposed from different studies. Our study demonstrated that quercetin acted as an antioxidant in HepG2 cells when cells were treated with 10 and 100 micromol/L quercetin for 30 min, but quercetin acted as a pro-oxidant when cells were incubated at 100 micromol/L quercetin for longer periods (12 and 24 h). Quercetin is capable of reducing H(2)O(2)-induced oxidative stress of HepG2 cells through different mechanisms, such as detoxification of H(2)O(2,) inhibition of ROS generation, and removal of generated ROS. We find that quercetin can block ROS generation through Fenton reaction to produce hydroxyl radicals by chelating with transition metal ions such as Cu(2+). Evidence that quercetin might exert an antioxidant effect by changing generated ROS into less reactive ROS suggests that when quercetin reacts with ROS, it becomes oxidized, which is less harmful but still reactive, and the oxidized quercetin interacts with thiol compounds as reduced GSH to return to the parent compound quercetin. In contrast, the prolonged treatment of quercetin in high concentrations (100 micromol/L) shows that quercetin may act as a pro-oxidant rather than as an antioxidant, resulting in cell death (apoptosis).