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.

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.

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.

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.

Antioxidant and pro-oxidant effects of green tea extracts in oxygen radical absorbance capacity assay.

Green tea extracts (GTEs) [water (GTE-W) and 75% ethanol (GTE-E)] were investigated to characterize their propensities to act as antioxidants or as pro-oxidants by analyzing oxygen radical absorbance capacity (ORAC) and scavenging capacity for hydroxyl radical. When 2,2'-azobis(2-amidinopropane) dihydrochloride was used for the generation of peroxyl radicals, both GTE-W and GTE-E exhibited strong concentration-dependent scavenging activity through donating protons, which could be explained by their reducing property. When hydroxyl radicals were generated through the addition of Cu(2+) and H(2)O(2), GTE-W and GTE-E exhibited antioxidant activity or pro-oxidant activity, depending on their concentrations, which might be attributed to the metal chelating activity, the scavenging activity on hydroxyl radical, and/or the pro-oxidant activity to generate some reactive oxygen species. When Cu(2+) without H(2)O(2) was used as an oxidant in the assay, the copper-initiated pro-oxidant activities of GTE-W and GTE-W was consistent with the availability of (-)-epigallocatechin and (-)-epicatechin to generate hydrogen peroxide and/or hydroxyl radical. The pro-oxidant activity of GTE-W and GTE-E was demonstrated by the deoxyribose assay. These results indicate that both GTE-W and GTE-E can have pro-oxidant activity at lower concentrations and antioxidant activity at higher concentrations in the ORAC and deoxyribose assays using generated hydroxyl radicals.