Antioxidant and Skin Whitening Activities of Sub- and Super-Critical Water Treated Rutin.

We focused on the functional components, antioxidant activity, skin-whitening, and anti-wrinkle properties of subcritical and supercritical water (SCW)-treated rutin. Rutin treatments were performed at the following temperature and pressure conditions: 200 °C/15 bar, 300 °C/100 bar, and 400 °C/250 bar. ABTS and DPPH radical scavenging activities and reducing power presented their highest values (1193.72 mg AAE/g, 728.73 mg AAE/g, and 0.65, respectively) at 300 °C/100 bar. The tyrosinase inhibitory activity of SCW-treated rutin was 21.72-60.05% at 1 mg/mL. The ethyl acetate fraction showed 14.91% melanin inhibitory activity at a concentration of 10 µg/mL compared to the α-MSH treatment group. The protein expression inhibition rates of MITF, tyrosinase, TRP-1, and TRP-2 in the ethyl acetate fractions were 14.05%, 72%, 93.05%, and 53.44%, respectively, at a concentration of 10 µg/mL, compared to the control. These results indicate that SCW treatment could be used to develop cosmetic materials and functional food with physiological activity, and that SCW-treated rutin can be used as a skin-whitening cosmetic material.

Effect of sorghum ethyl-acetate extract on benign prostatic hyperplasia induced by testosterone in Sprague-Dawley rats.

Benign prostatic hyperplasia (BPH) is commonly observed in men > 50 years worldwide. Phytotherapy is one of the many treatment options. Sorghum (Sorghum bicolor L.) contains various health-improving phytochemicals with antioxidant and inhibitory activities on cell proliferation, both in vitro and in vivo. To confirm the effects of Donganme sorghum ethyl-acetate extract (DSEE) on BPH, we induced BPH in Spragye-Dawley rats using exogenous testosterone. We measured prostate weight, examined prostrates histopathologically, and analyzed mRNAs associated with male hormones and proteins associated with cell proliferation in the prostate. DSEE inhibited weight gain of the prostate; decreased mRNA expressions of androgen receptor and 5α-reductase II; and improved histopathological symptoms, the protein-expressed ratio of Bax/Bcl-2, and the oxidative status of BPH induced by testosterone in SD rats. Therefore, DSEE may have potential as a preventive or therapeutic agent against BPH.

A silk peptide fraction restores cognitive function in AF64A-induced Alzheimer disease model rats by increasing expression of choline acetyltransferase gene.

This study investigated the effects of a silk peptide fraction obtained by incubating silk proteins with Protease N and Neutrase (SP-NN) on cognitive dysfunction of Alzheimer disease model rats. In order to elucidate underlying mechanisms, the effect of SP-NN on the expression of choline acetyltransferase (ChAT) mRNA was assessed in F3.ChAT neural stem cells and Neuro2a neuroblastoma cells; active amino acid sequence was identified using HPLC-MS. The expression of ChAT mRNA in F3.ChAT cells increased by 3.79-fold of the control level by treatment with SP-NN fraction. The active peptide in SP-NN was identified as tyrosine-glycine with 238.1 of molecular weight. Male rats were orally administered with SP-NN (50 or 300mg/kg) and challenged with a cholinotoxin AF64A. As a result of brain injury and decreased brain acetylcholine level, AF64A induced astrocytic activation, resulting in impairment of learning and memory function. Treatment with SP-NN exerted recovering activities on acetylcholine depletion and brain injury, as well as cognitive deficit induced by AF64A. The results indicate that, in addition to a neuroprotective activity, the SP-NN preparation restores cognitive function of Alzheimer disease model rats by increasing the release of acetylcholine.

Effect of the Capsicoside G-rich Fraction from Pepper (Capsicum annuum L.) Seeds on High-fat Diet-induced Obesity in Mice.

Obesity is one of the most common metabolic syndromes and is a major threat to human health worldwide. Given the size of this problem, there is growing interest in natural agents that may decrease obesity. In this study, we investigated the anti-obesity effect of a capsicoside G-rich fraction (CRF; 13.35% capsicoside G) isolated from pepper seeds in diet-induced obese mice. C57BL/6J mice were fed either a normal diet or a high-fat diet (HFD), with or without CRF (HFD + CRF; 10 and 100 mg/kg body weight). The body weight and food efficiency ratio of mice fed HFD + CRF were lower in comparison to that of mice fed only an HFD. Epididymal adipose tissue weight and adipocyte hypertrophy were significantly lower in HFD + CRF mice than in HFD mice. The fat deposition in the liver of mice fed HFD + CRF was lower compared to that of mice fed only an HFD. CRF significantly reversed the HFD-induced elevation of the expression of key adipocyte differentiation regulators, including peroxisome proliferator-activated receptor γ, CCAAT/enhancer-binding protein α, sterol regulatory element binding protein 1c, and their target genes. These results suggest that CRF could be used as dietary therapy for the prevention of obesity and obesity-related metabolic diseases. Copyright © 2016 John Wiley & Sons, Ltd.

(E)-2,4-Bis(p-hydroxyphenyl)-2-butenal inhibits tumor growth via suppression of NF-κB and induction of death receptor 6.

The Maillard reaction products are known to be effective in chemoprevention. Here, we focused on the anti-cancer effects of (E)-2,4-bis(p-hydroxyphenyl)-2-butenal on in vitro and in vivo colon cancer. We analysed the anti-cancer activity of (E)-2,4-bis(p-hydroxyphenyl)-2-butenal on colon cancer cells by using cell cycle and apoptosis analysis. To elucidate it's mechanism, NF-κB DNA binding activity, docking model as well as pull-down assay. Further, a xenograft model of colon cancer was studied to test the in vivo effects of (E)-2,4-bis(p-hydroxyphenyl)-2-butenal. (E)-2,4-Bis(p-hydroxyphenyl)-2-butenal inhibited colon cancer cells (SW620 and HCT116) growth followed by induction of apoptosis in a concentration-dependent manner via down-regulation of NF-κB activity. In docking model as well as pull-down assay, (E)-2,4-bis(p-hydroxyphenyl)-2-butenal directly binds to three amino acid residues of IKKß, thereby inhibited IKKß activity in addition to induction of death receptor 6 (DR6) as well as their target apoptotic genes. Finally, (E)-2,4-bis(p-hydroxyphenyl)-2-butenal suppressed anchorage-independent cancer cell growth, and tumor growth in xenograft model accompanied with apoptosis through inhibition of IKKß/NF-κB activity, and overexpression of DR6. These results suggest that (E)-2,4-bis(p-hydroxyphenyl)-2-butenal inhibits colon cancer cell growth through inhibition of IKKß/NF-κB activity and induction of DR6 expression.

Anti-inflammatory effect of tricin 4'-O-(threo-ß-guaiacylglyceryl) ether, a novel flavonolignan compound isolated from Njavara on in RAW264.7 cells and in ear mice edema.

Although recent study has shown tricin 4'-O-(threo-ß-guaiacylglyceryl) ether (TTGE), an isolated compound from Njavara rice, to have the most potent anti-inflammatory effects, the action mechanism has not been fully understood. Here, we examined the effect of TTGE on the inflammation and elucidated the potential mechanism. We demonstrated that TTGE significantly inhibited LPS-induced NO and ROS generation in RAW264.7 cells, which was correlated with the down-regulating effect of TTGE on the iNOS and COX-2 expression via NF-κB and STAT3. TPA-induced ear edema was also efficiently inhibited by the TTGE treatment. TTGE blocked the induction of iNOS and COX-2 through the regulation of NF-κB and STAT3, which could explain the reduced TPA-induced edema symptoms. Moreover, the introduction of ERK inhibitor abrogated the anti-inflammatory effect of TTGE via the recovery of NF-κB and STAT3 signalings. Taken together, these results suggest that TTGE has anti-inflammatory properties through down-regulation of NF-κB and STAT3 pathways.

Protective Effect of Whole Wheat on Muscle Atrophy in C2C12 Cells via Akt/FoxO1 Signaling Pathways.

Skeletal muscles are important for body movement, postural maintenance, and energy metabolism. Muscle atrophy is caused by various factors, including lack of exercise, age, genetics, and malnutrition, leading to the loss of muscle mass. The Akt/FoxO signaling pathway plays a key role in the regulation of muscle protein synthesis and degradation. Whole wheat contains functional ingredients that may indirectly contribute to muscle health and function and can help prevent or slow the progression of muscle atrophy. In this study, the protective effects of three wheat cultivars (Seodun, Ol, and Shinmichal 1) against hydrogen peroxide-induced muscle atrophy in C2C12 cells were investigated. We found that whole-wheat treatment reduced reactive oxygen species production, prevented glutathione depletion, and increased myotube diameter, thereby reducing muscle atrophy by activating myoblast differentiation. Generally, "Shinmichal 1" exhibited the highest activation of the Akt/FoxO signaling pathway. In contrast, "Seodun" showed similar or slightly higher activities than those of the H2O2-treated only group. In conclusion, whole wheat exerts a protective effect against muscle atrophy by activating the Akt/FoxO signaling pathway. This study indicates that whole wheat may help prevent muscle atrophy.

Protective Effects of Cereal Grain Extracts on Alcohol-Induced Hepatocyte Damage.

This study investigated the protective effects of cereal grains on alcohol-induced hepatocyte damage. Cereal grains were extracted with methanol, and their radical scavenging properties and total phenolic contents were examined. Black rice extract exhibited the highest total polyphenol content and radical scavenging capacity. Treatment with sorghum extract increased the viability of cells exposed to alcohol by up to 81.6%. All cereal grain extracts decreased reactive oxygen species and malondialdehyde production and glutathione depletion in HepG2 cells exposed to ethanol. In particular, black rice and sorghum extracts exhibited greater antioxidant effects than other cereal grains. Treatment with black rice extract increased the levels of alanine aminotransferase and aspartate aminotransferase of alcohol-exposed cells to control levels. Overall, black rice extract showed a greater protective effect compared with other cereal grains against alcohol exposure in HepG2 cells and could improve alcohol-induced liver problems.

Physicochemical Properties of Soft and Hard-type Rice Flour According to Moisture Content and High Hydrostatic Pressure Treatment.

This study investigated the effects of high hydrostatic pressure (HHP) treatment on the physicochemical properties of rice flour according to its moisture levels in order to develop new materials for processed rice foods. The rice varieties used were the Samkwang variety (normal and hard type) and the Shingil variety (processing and soft type). The moisture content of the rice flour was adjusted to 35-55% and it was treated with the HHP treatment at 400-600 MPa. The water absorption capacity, solubility, and swelling power of the rice flour increased as the moisture levels and pressure increased. The 600 MPa enzymatic hydrolysis-treated rice flour showed similar results to the heat-treated rice flour. Scanning electron microscopy showed few cavities, resulting in a dense structure. X-ray diffraction confirmed that the 23° peak, which indicates the degree of gelatinization, decreased with increasing moisture levels and pressure. The HHP treatment of the rice flour changed its physicochemical properties according to the moisture levels and pressure applied. These results can provide important information on the development and production of various foods.

Sucrose-induced abiotic stress improves the phytochemical profiles and bioactivities of mung bean sprouts.

This study aimed to examine the impact of sucrose treatment on the growth conditions, dietary nutritional quality, and biological activities of mung bean sprouts. Mung bean seeds were sprouted with solutions containing different sucrose concentrations (10, 20, and 30 g/L). The application of exogenous sucrose significantly decreased the height and fresh weight of mung bean sprouts. However, the sucrose-treated sprouts contained more polyphenols, flavonoids, γ-aminobutyric acid, phytosterols, and vitamins. The antioxidant capacities were also significantly higher in the sucrose-treated sprouts than in the control sprouts. The sprouts treated with 2-3 % sucrose showed markedly improved FFA-induced insulin resistance and alcohol-induced oxidative injury in HepG2 cells. Taken together, the elicitor application of sucrose at 3 % during mung bean sprouting could be an effective strategy to improve the dietary phytochemical composition and provide potential health benefits.

Unsaponifiable Matter from Wheat Bran Cultivated in Korea Inhibits Hepatic Lipogenesis by Activating AMPK Pathway.

Unsaponifiable matter (USM) from wheat bran, a by-product obtained from wheat milling, is abundant in health-promoting compounds such as phytosterols, tocopherols, policosanols, and alkylresorcinols. This study aimed to examine the effects of USM from the wheat bran of normal and waxy type wheat, Saekeumkang (SKK) and Shinmichal (SMC), on hepatic lipid accumulation in free fatty acid (FFA)-induced hepatocytes and to investigate the cellular mechanism. The total phytochemical contents were 46.562 g/100 g USM and 38.130 g/100 g USM from SKK and SMC, respectively. FFA treatment increased intracellular lipid accumulation by approximately 260% compared to the control group; however, treatment with USM from SKK and SMC significantly attenuated lipid accumulation in the hepatocytes in a dose-dependent manner. Moreover, USM downregulated the expression of lipogenic factors such as fatty acid synthase and sterol regulatory-element-binding protein 1c by approximately 40% compared to the FFA treatment group. Treatment with USM promoted lipolysis and positively regulated the expression of the proteins involved in ß-oxidation, including peroxisome proliferator-activated receptor α and its downstream protein, carnitine palmitoyltransferase 1A. Moreover, the blockade of AMPK activation significantly abolished the inhibitory effects of USM on hepatic lipid accumulation. These results indicated that the USM from both SKK and SMC can alleviate lipid accumulation in hepatocytes in an AMPK-dependent manner. Therefore, USM from wheat bran may be useful as a therapeutic intervention for treating metabolic-dysfunction-associated fatty liver disease.

Fermentation and Quality Characteristics of Yogurt Treated with Bifidobacterium longum.

The fermentation and quality characteristics of yogurt were investigated according to the inoculation concentration of Bifidobacterium longum. The total sugar content of yogurt decreased as the fermentation time increased, and with an increased concentration of B. longum treatment the fermentation time decreased rapidly. As fermentation progressed, the lactose content decreased rapidly at the beginning and gradually decreased as the pH decreased. Depending on the B. longum treatment concentration, the lactose content varied from 0.29 ± 0.01 to 0.47 ± 0.01% and was 0.5% or less in all experimental groups. The experimental group inoculated with 0.0015% of B. longum displayed the best results in all categories, including pH, total acidity, lactic acid content, solid non-fat content, and total lactic acid bacteria count, which are factors that determine the quality of yogurt. In summary, the experimental group inoculated with 0.0015% of B. longum was determined to be the highest quality yogurt.

Quality Characteristics of Sweet Potato Jelly Prepared Using the Enzymatic Saccharification Method.

In this study, jelly was prepared using saccharified sweet potatoes without sugar, and its quality characteristics were compared according to the sweet potato cultivar. Three sweet potato varieties, namely Juwhangmi (orange color), Sinjami (purple color), and Daeyumi (yellow flesh color), were used. The total free sugar and glucose contents of the hydrolysate were found to increase during the enzyme treatment. However, no differences in the moisture, total soluble solids, or textural properties were found among the sweet potato cultivars. Sinjami had high total polyphenol and flavonoid contents of 446.14 mg GAE/100 g and 243.59 mg CE/100 g, respectively, and it had the highest antioxidant activity among the cultivars. Based on the sensory evaluation, an overall preference appeared in the order of Daeyumi, Sinjami, and Juwhangmi cultivars. This result shows that jelly can be manufactured by saccharifying sweet potatoes, and it was confirmed that the characteristics of raw sweet potatoes had a great influence on the quality characteristics of the jelly. Further, the characteristics of raw sweet potatoes had a remarkable influence on the quality characteristics of the jelly.

Antioxidative and Anti-Inflammatory Activities of Rosebud Extracts of Newly Crossbred Roses.

Oxidative stress and inflammation are basic pathogenic factors involved in tissue injury and pain, as well as acute and chronic diseases. Since long-term uses of synthetic steroids and non-steroidal anti-inflammatory drugs (NSAIDs) cause severe adverse effects, novel effective materials with minimal side effects are required. In this study, polyphenol content and antioxidative activity of rosebud extracts from 24 newly crossbred Korean roses were analyzed. Among them, Pretty Velvet rosebud extract (PVRE) was found to contain high polyphenols and to show in vitro antioxidative and anti-inflammatory activities. In RAW 264.7 cells stimulated with lipopolysaccharide (LPS), PVRE down-regulated mRNA expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), and thereby decreased nitric oxide (NO) and prostaglandin E2 (PGE2) production. In a subcutaneous air-pouch inflammation model, treatment with PVRE decreased λ-carrageenan-induced tissue exudation, infiltration of inflammatory cells, and inflammatory cytokines such as tumor necrosis factor-α and interleukin-1ß concentrations, as achieved with dexamethasone (a representative steroid). Notably, PVRE also inhibited PGE2, similar to dexamethasone and indomethacin (a representative NSAID). The anti-inflammatory effects of PVRE were confirmed by microscopic findings, attenuating tissue erythema, edema, and inflammatory cell infiltration. These results indicate that PVRE exhibits dual (steroid- and NSAID-like) anti-inflammatory activities by blocking both the iNOS-NO and COX-2-PG pathways, and that PVRE could be a potential candidate as an anti-inflammatory material for diverse tissue injuries.

2,4-bis (p-hydroxyphenyl)-2-butenal (HPB242) induces apoptosis via modulating E7 expression and inhibition of PI3K/Akt pathway in SiHa human cervical cancer cells.

The Maillard reaction is a chemical reaction occurring between an amino acid and a reducing sugar, usually requiring thermal processing. Maillard reaction products (MRPs) have antioxidant, antimutagenic, and antibacterial effects, and although 2,4-bis (p-hydroxyphenyl)-2-butenal (HPB242), a fructose-tyrosine MRP, appears to inhibit proliferation of cancer cells, its mechanism of action has not been studied in detail. We found that HPB242 treatment modulated expression of cyclins and tumor suppressor genes in SiHa human cervical cancer cell lines: cyclins and phospho-pRB were downregulated, whereas the expression of CDK inhibitors and p53 was enhanced. HPB242 induced apoptosis dose-dependently by suppressing E7 expression and leading to sub-G1 cell-cycle arrest in SiHa cell lines; treatment also led to the proteolytic cleavage of caspase-3, -9, and poly (ADP-ribose) polymerase. Moreover, HPB242 upregulated Fas expression, altered expressions of pro- and antiapoptotic factors, and also inhibited nuclear translocation of nuclear factor κB and phosphorylation of IκB. HPB242 treatment decreased phosphatidyl inositol-3 kinase and p-Akt expression levels, demonstrating that this survival pathway may also be inhibited by HPB242. Cumulatively, HPB242 promotes apoptosis by influencing E7 expression, inducing cell-cycle arrest at sub-G1 phase, and promoting both intrinsic (mitochondrial) and extrinsic (Fas-dependent) apoptosis in SiHa human cervical cancer cells.

Antiobesity effects of a sulfur compound thiacremonone mediated via down-regulation of serum triglyceride and glucose levels and lipid accumulation in the liver of db/db mice.

Garlic is widely used as a spice. Garlic extracts exert anticancer and antiinflammatory effects, but its antiobesity efficacy studies have produced conflicting results. The antiobesity effects of thiacremonone, a sulfur compound isolated from garlic, was evaluated in obese db/db mice. Thiacremonone was orally administrated to mice for 3 weeks. The thiacremonone-treated db/db mice showed a loss of body weight and decrease in blood triglyceride and glucose levels compared with the control mice. Histological analysis further revealed that thiacremonone significantly decreased lipid accumulation in the fatty livers of treated db/db mice. It was observed that GLUT-4 expression and glucose uptake were up-regulated by thiacremonone in 3T3-L1 adipocytes. Thiacremonone treatment also suppressed expression levels of acetyl-CoA carboxylase (ACC) and fatty acid synthase (FAS), which are involved in lipid metabolism, in the liver of db/db mice. In addition, thiacremonone enhanced peroxisome proliferator-activated receptor γ (PPARγ) expression in the fatty liver. Taken together, these results suggest that thiacremonone may play a vital role in improving the management of obesity and related metabolic syndromes via inhibition of lipid accumulation.

Antioxidant and Cytoprotective Capacities of Various Wheat (Triticum aestivum L.) Cultivars in Korea.

Whole wheat (Triticum aestivum L.) is a rich source of bioactive compounds with health benefits such as antioxidant, anti-inflammatory, and anti-proliferative activities. In this study, we evaluated the antioxidant and cytoprotective capacities of 41 wheat cultivars. The antioxidant capacities of whole wheat grain extracts (WWE) from various wheat cultivars were evaluated using total phenolic content and ABTS and DPPH radical-scavenging activities. The relative antioxidant capacity index (RACI) was calculated to integrate different chemical methods of antioxidant capacity. The cytoprotective capacity of the WWE was investigated using hepatocytes (HepG2), myoblasts (C2C12), and endothelial (EA.hy926) cells. The RACI was the highest and lowest for Dajoong (1.71) and Topdong (-1.96), respectively. Pearson correlation tests were conducted to determine the correlation between the antioxidant and cytoprotective activities. However, no significant correlations between RACI and the cytoprotective capacities were ascertained. Principal component analysis revealed that the first two components represented 68.93% of the total variability. Hierarchical cluster analysis classified WWE into three groups based on measured parameters. The results of this study highlight the variation in the antioxidant and cytoprotective capacities of 41 different wheat cultivars. This study provides basic information that can guide decisions in wheat breeding programs for the development of functional food crops and new dietary ingredients.

Biological activities of sweet potato (Ipomoea batatas L.) tips and tubers.

This study was conducted to evaluate the biological activities of sweet potato tips and tubers. Antioxidant activity of 2,2-azino-bis 93-ethlbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS) and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activities had the highest value of 32.45 mg, AAE/g, and 15.10 mg AAE/g, respectively, in 'Pungwonmi' tips. Angiotensin converting enzyme I inhibitory activity ranged between 47.72% in 'Sinjami' tubers and 62.25% in 'Pungwonmi' tips. α-Glucosidase inhibitory activity had the highest value of 78.81% and 62.93% in 'Pungwonmi' tips and 'Juhwangmi' tubers, respectively. In particular, 'Pungwonmi' tips had the most effective inhibiting effect on intracellular reactive oxygen species levels in HepG2 cells. Wound healing assay result revealed that 'Sinjami' showed 75% wound healing effect. For skin whitening, 'Pungwonmi' tips showed 63% activity at 10 mg/ml. These results suggest that sweet potato tips and tubers can be used to develop functional food and cosmetic materials.

Inhibitory effect of a tyrosine-fructose Maillard reaction product, 2,4-bis(p-hydroxyphenyl)-2-butenal on amyloid-ß generation and inflammatory reactions via inhibition of NF-κB and STAT3 activation in cultured astrocytes and microglial BV-2 cells.

BACKGROUND: Amyloidogenesis is linked to neuroinflammation. The tyrosine-fructose Maillard reaction product, 2,4-bis(p-hydroxyphenyl)-2-butenal, possesses anti-inflammatory properties in cultured macrophages, and in an arthritis animal model. Because astrocytes and microglia are responsible for amyloidogenesis and inflammatory reactions in the brain, we investigated the anti-inflammatory and anti-amyloidogenic effects of 2,4-bis(p-hydroxyphenyl)-2-butenal in lipopolysaccharide (LPS)-stimulated astrocytes and microglial BV-2 cells. METHODS: Cultured astrocytes and microglial BV-2 cells were treated with LPS (1 µg/ml) for 24 h, in the presence (1, 2, 5 µM) or absence of 2,4-bis(p-hydroxyphenyl)-2-butenal, and harvested. We performed molecular biological analyses to determine the levels of inflammatory and amyloid-related proteins and molecules, cytokines, Aß, and secretases activity. Nuclear factor-kappa B (NF-κB) DNA binding activity was determined using gel mobility shift assays. RESULTS: We found that 2,4-bis(p-hydroxyphenyl)-2-butenal (1, 2, 5 µM) suppresses the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) as well as the production of nitric oxide (NO), reactive oxygen species (ROS), tumor necrosis factor-α (TNF-α), and interleukin-1ß (IL-1ß) in LPS (1 µg/ml)-stimulated astrocytes and microglial BV-2 cells. Further, 2,4-bis(p-hydroxyphenyl)-2-butenal inhibited the transcriptional and DNA binding activity of NF-κB--a transcription factor that regulates genes involved in neuroinflammation and amyloidogenesis via inhibition of IκB degradation as well as nuclear translocation of p50 and p65. Consistent with the inhibitory effect on inflammatory reactions, 2,4-bis(p-hydroxyphenyl)-2-butenal inhibited LPS-elevated Aß42 levels through attenuation of ß- and γ-secretase activities. Moreover, studies using signal transducer and activator of transcription 3 (STAT3) siRNA and a pharmacological inhibitor showed that 2,4-bis(p-hydroxyphenyl)-2-butenal inhibits LPS-induced activation of STAT3. CONCLUSIONS: These results indicate that 2,4-bis(p-hydroxyphenyl)-2-butenal inhibits neuroinflammatory reactions and amyloidogenesis through inhibition of NF-κB and STAT3 activation, and suggest that 2,4-bis(p-hydroxyphenyl)-2-butenal may be useful for the treatment of neuroinflammatory diseases like Alzheimer's disease.

Protective Activity and Underlying Mechanism of Ginseng Seeds against UVB-Induced Damage in Human Fibroblasts.

Ginseng seeds are rich in phytosterols, ginsenosides, and fatty acids, and can therefore be used in skincare to delay the aging process. Ginseng seed embryo (GSE) and ginseng seed coat (GSC) were separated from ginseng seeds (Panax ginseng Meyer). This study evaluated the protective activity and underlying mechanism of GSE and GSC on UVB irradiation-induced skin photoaging using Hs68 cells. Their bioactive compounds, including phytosterols, ginsenosides, tocopherols, tocotrienols, and fatty acids were determined by HPLC and GC. The levels of reactive oxygen species, matrix metalloproteinases (MMPs), and collagen levels were measured in human dermal fibroblast cell line, Hs68 cells. The antioxidant capacity and contents of total polyphenols and flavonoids were higher in GSC than those in GSE. Linoleic acid was the major fatty acid in both GSE and GSC. GSE and GSC treatment alleviated UVB-induced increase of reactive oxygen species (ROS), matrix metalloproteinase (MMP)-1, and MMP-3, resulting in reduced collagen degradation. Increased UVB-mediated phosphorylation of mitogen activated protein kinase (MAPK) and activator protein-1 (AP-1) was inhibited by GSE and GSC treatment. Moreover, GSE and GSC effectively upregulated transforming growth factor-ß (TGF-ß) 1 levels. It was found that ginseng seeds regulate the expression of TGF-ß/Smad and MAPK/AP-1 pathways. Ginseng seeds contain various bioactive compounds and have protective activity against UVB-induced skin photoaging. Therefore, ginseng seeds have the potential for use in cosmeceutical preparations.