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Hepatitis C virus (HCV) infection is a significant health problem, with a worldwide prevalence of about 170 million. Recently, the development of direct acting antiviral (DAA) as a therapeutic agent for HCV has been rapidly increasing. However, DAA has a side effect and is costly. Therefore, it is still necessary to develop a therapeutic agent to treat HCV infection using products. Agrimonia pilosa (AP) and Galla rhois (RG) are traditional medicines and are known to display therapeutic activity on various diseases. Notably, they have been reported to have an anti-viral effect on HBV and influenza virus infections. It is expected that anti-viral activity will increase when two extracts are mixed. To investigate their anti-viral activity, the expression level of HCV Core 1b and NS5A was measured. Remarkably, AP, RG, and their mixed compound (APRG64) strongly inhibited the expression of viral proteins, which led us to identify their metabolites. A total of 14 metabolites were identified using liquid chromatography mass spectrometry (LC-MS). These metabolites were evaluated for their anti-HCV activity to identify active ingredients. In conclusion, our results unveiled that anti-HCV activity of Agrimonia pilosa and Galla rhois extract mixture could lead to the development of a novel therapy for HCV infection.

Lilium Asiatic hybrids (Lilium spp.) are produced by interspecific crosses of Sinomartagon species belonging to Liliaceae. To date, no phytochemical work appears to have been conducted on Lilium Asiatic hybrids. In the current work, solvent extraction, solvent fractionation, and repeated SiO2 and ODS column chromatography yielded three new steroidal saponins along with a known one, avenacoside A (1). The chemical structures of the new saponins were determined based on extensive spectroscopic methods as well as chemical and biological reactions to be 26-O-β-D-glucopyranosylnuatigenin 3-O-α- l -rhamnopyranosyl-(1 → 2)-O-[(4-O-methyl)-β- d -glucopyranosyl-(1 → 6)-β- d -glucopyranosyl-(1 → 4)]-β- d -glucopyranoside (2), 26-O-β-D-glucopyranosylnuatigenin 3-O-β- d -glucopyranosyl-(1 → 4)-α- l -rhamnopyranosyl-(1 → 2)-(6-acetoxyl)-β- d -glucopyranoside (3), and 26-O-β-D-glucopyranosylnuatigenin 3-O-β- d -glucopyranosyl-(1 → 2)-O-[β- d -glucopyranosyl-(1 → 6)]-β- d -glucopyranoside (4), named lilyasiasides A-C, respectively. The aglycone of the saponins, a nuatigenin, is an atypical spirostanol sapogenin possessing a pentacyclic F-ring, furospirostane steroid, which is very rarely occurred in Lilium species.

Our previous study we isolated novel bacterial stain, Epidermidibacterium keratini, called EPI-7T from skin samples. Repeated column separation yielded one new pyrimidine compound, 1,1′-biuracil, from EPI-7T culture solutions grown in R2A medium. Its chemical structure was determined based on spectroscopic data, IR, FAB/MS, and NMR. And 1,1′-biuracil and EPI-7T culture solutions showed regulating effects of anti-aging associated mRNA expressions in UV-irradiated fibroblasts without toxicity in Hs68 cells. These results demonstrates the cosmetic potential of 1,1′-biuracil and EPI-7T as anti-aging agents.

Malva verticillata (Chinese mallow) has long been used in traditional medicines and herbal teas in Asia. The n-BuOH fraction (Fr) from M. verticillata promoted significant recovery of alloxan-damaged (AXD) pancreatic islets (PIs) in zebrafish (ZF). Two major components were isolated from M. verticillata through repeated-column chromatography. Based on several spectroscopic methods, including nuclear magnetic resonance (NMR), infrared spectroscopy (IR), and fast atom bombardment-mass spectrometry (FAB-MS), the chemical structures of compounds 1 and 2 were determined. In addition, the quantity of both compounds in the n-BuOH Fr was investigated through high-performance liquid chromatography (HPLC) and the quantities of compounds 1 and 2 in the n-BuOH Fr were determined to be 5.58% ± 0.16% and 2.85% ± 0.13%, respectively. The n-BuOH Fr, compounds 1 and 2, and the mixture of compounds 1 and 2 (MX, 1 and 2, the ratio of both compounds in n-BuOH Fr, 1.96:1) were evaluated for their ability to recover AXD PIs and for their KATP channel-blocking mechanism using diazoxide in ZF. The n-BuOH Fr (10 μg/mL) and compounds 1 and MX (1 μg/mL) exhibited a recovery effect on AXD PIs. The n-BuOH Fr (10 μg/mL) and MX (1 μg/mL) were also confirmed to be useful KATP channel activators. A synergistic effect of MX in the recovery of AXD PIs was first confirmed in ZF, and it was discovered that 2 acted as an insulin sensitivity activator that increased the activity of compound 1.

Breast-fed infants have Bifidobacterium-rich gut microbiota compared to infants fed formula. Fucosylated oligosaccharides are the major components of human milk oligosaccharide (HMO) which confer various beneficial effects including prebiotic effect and protection from pathogenic infection on the host. A novel prebiotics was developed using bifidobacterial β-galactosidase and fucose and lactose as substrates. Structure analysis revealed it as β-D-galactopyranosyl-(1 → 3)-O-L-fucopyranose named as β-galactosyl fucose (gal-fuc), which is different from common fucosylated HMOs with α1-2, α1-3, and α1-4 linkages. Among the four Lactobacillus strains examined, all but L. delbrueckii subsp. bilgaricus KCTC 3635 grew better on gal-fuc than on β-GOS. Among the 11 bifidobacterial species examined, all except for B. bifium used gal-fuc as much as GOS. Moreover, the gal-fuc was noticeably better used by Bifidobacterium infantis, the major intestinal bacteria of breast fed infant. Among 15 non-probiotic bacteria, only 4 strains used gal-fuc better than β-GOS. In conclusion, a novel gal-fuc is expected to contribute to beneficial changes of gut microbiota. Graphical abstract A novel form of β-galactosyl fucose with an improved prebiotic effect.

Colloidal quantum-dot based light-emitting diodes (QD-LEDs) are attractive for use in display devices because of the remarkable electrical and optical characteristics of colloidal quantum dots. An inverted structure may be one method to achieve the necessary multilayer device structures in QD-LEDs. In this study, each layer of an inverted-structure QD-LED was optimized. The effect of the solvent on the hole transfer layer was investigated, along with the effect of the concentration of the electron transfer layer, the effect of the co-solvent on the hole transfer layer, and the effect of the concentration and solvent of quantum dot layer. The quantum dots and ZnO NPs were synthesized as the emitting layer and carrier transporting layer using a solution-mediated process. The inverted QD-LED device showed a luminance of 3,762 cd/m², current efficiency of 1.86 cd/A, and EQE of 1.18%.

We synthesized medium-band-gap donor-acceptor (D-A) -type conjugated polymers (PBTZCZ-L and PBTZCZ-H) consisting of a benzotriazole building block as an acceptor and a carbazole unit as a donor. In comparison with the polymers, a small conjugated molecule (BTZCZ-2) was developed, and its structural, thermal, optical, and photovoltaic properties were investigated. The power conversion efficiency (PCE) of the BTZCZ-2-based solar cell devices was less than 0.5%, considerably lower than those of polymer-based devices with conventional device structures. However, inverted solar cell devices configured with glass/ITO/ZnO:PEIE/BTZCZ-2:PC71BM/MoO3/Ag showed a tremendously improved efficiency (PCE: 5.05%, Jsc: 9.95 mA/cm2, Voc: 0.89 V, and FF: 57.0%). We believe that this is attributed to high energy transfer and excellent film morphologies.

The production of soybean continues to increase worldwide. People are showing more interest in the beneficial health effects of soybeans than before. However, the origin and history of soybeans are still being discussed among many researchers. Chromatographic methods enable the desirable separation of a variety of isoflavones from soybeans. The structures of isolated soy isoflavones have been successfully identified in tandem with spectroscopic analytical instruments and technologies such as liquid chromatography, mass spectrometry, and nuclear magnetic resonance spectroscopy. The theoretical background behind spectroscopy may help improve the understanding for the analysis of isoflavones in soybeans and soy-derived foods. This review covers the origin of the English name of soybean and its scientific name

Amylosucrase (ASase, EC.4.2.1.4) is well-known for its distinguishable property of transglycosylation of many flavonoids and phenolics. Quercetin has diverse biological functions, however, its use is limited due to poor solubility and bioavailability. ASase derived from Deinococcus geothermalis (DGAS) showed conditional preference for producing unusual quercetin glucosides (QGs). DGAS produced a variety of QGs including quercetin monoglucosides (QG1), diglucosides (QG2 and QG2′), and triglucoside from quercetin and sucrose. The newly synthesized QG2′ was recognized as a novel quercetin isomaltoside with an α-1,6 linkage branched at the − OH of C4′ in quercetin by mass and nuclear magnetic resonance spectra. With a higher conversion yield from quercetin to QGs (60-92%), the optimum conditions for producing QG2′ were examined under various pH and sucrose concentrations by response surface methodology (RSM). QG2′ was predominantly produced under acidic conditions (pH 5.0) and at high sucrose concentrations (1,000-1,500 mM). In contrast, QG1 was generated as an intermediate of consecutive glycosylation. Kinetic evaluations indicated that considerable differences of transglycosylation velocities were caused by the pH and buffer salts of the reaction, which had a 3.9-fold higher overall performance (kcat/K′m) of generating QG2′ at pH 5 compared to at pH 7. A rationale of unusual transglycosylations was demonstrated with a molecular docking simulation. Taken together, our study demonstrated that ASase can be used to synthesize unusually branched flavonoid glycosides from flavonol aglycones with clear patterns by modulating reaction conditions.

연꽃의 자방으로부터 80% MeOH로 추출하고, 얻어진 추출물을 n-hexane, ethyl acetate, n-butanol 및 H 2 O으로 용매 분획하였다. 이 중 n-hexane 분획물에 대해 silica gel과 octadecyl silica gel column chromatography 및 Prep-HPLC system을 반복 수행하여 5 종의 물질을 분리 하였다. 각 화합물의 화학구조는 NMR, ...

Although obovatol, a phenolic compound from the bark of Magnolia obovata, was known to have antioxidant, neuroprotective, antiinflammatory, antithrombotic and antitumour effects, its underlying antitumour mechanism is poorly understood so far. Thus, in the present study, the antitumour molecular mechanism of obovatol was investigated in non-small cell lung cancer cells (NSCLCs). Obovatol exerted cytotoxicity in A549 and H460 NSCLCs, but not in BEAS-2B cells. Also, obovatol increased sub-G1 accumulation and early and late apoptotic portion in A549 and H460 NSCLCs. Consistently, obovatol cleaved PARP, activated caspase 9/3 and Bax and attenuated the expression of cyclin D1 in A549 and H460 NSCLCs. Interestingly, obovatol upregulated the expression of endoplasmic reticulum stress proteins such as C/EBP homologous protein (CHOP), IRE1α, ATF4 and p-elF2 in A549 and H460 NSCLCs. Conversely, depletion of CHOP blocked the apoptotic activity of obovatol to increase sub-G1 accumulation in A549 and H460 NSCLCs. Overall, our findings support scientific evidences that obovatol induces apoptosis via CHOP activation in A549 and H460 NSCLCs. Copyright © 2016 John Wiley & Sons, Ltd.

Muscle regeneration is a coordinated process that involves proliferation and differentiation of muscle progenitor cells. Activation of MyoD is a key event in myogenic differentiation, which is regulated by p38 mitogen-activated protein kinases (MAPK). In a screen of natural compounds for the enhancement of MyoD activity, dehydrocorydaline (DHC) from the Corydalis tuber was identified. Treatment of C2C12 myoblasts with DHC increased the expression levels of muscle-specific proteins, including MyoD, myogenin and myosin heavy chain. In addition, C2C12 myoblasts exhibited enhanced multinucleated myotube formation without any cytotoxicity. Treatment with DHC elevated p38 MAPK activation and the interaction of MyoD with an E protein, which is likely to result in activation of MyoD and promotion of myoblast differentiation. Furthermore, defects in differentiation-induced p38 MAPK activation and myoblast differentiation induced by depletion of the promyogenic receptor protein Cdo in C2C12 myoblasts were restored by DHC treatment. In conclusion, these results indicated that DHC stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. These findings suggested that DHC may be considered a potential therapeutic compound for the improvement of muscle stem cell regenerative capacity in injured muscle.

The fruits of Prunus davidiana were extracted with 80 % aqueous methanol at room temperature. The concentrated extract was partitioned as ethyl acetate (EtOAc), n-butyl alcohol, and water fractions. From the EtOAc fraction, three triterpenoids were isolated through the repeated silica gel (SiO2) and octadecyl SiO2 column chromatographies. Based on physico-chemical and spectroscopic data including nuclear magnetic resonance, mass spectrometry, and infrared, the compounds were identified to be ursolic acid (1), corosolic acid (2), and α-amyrin (3).

The leaves of eggplant (Solanum melongena L.) were extracted with 80 % aqueous MeOH, and the concentrated extract was partitioned with n-hexane, EtOAc, n-BuOH, and water fractions. From the n-BuOH fraction, five compounds were isolated through the repeated silica gel, octadecyl silica gel, and Sephadex LH-20 column chromatographies. On the basis of physic-chemical and spectroscopic data including mass spectrometry, infrared spectroscopy, and nuclear magnetic resonance, they were identified to be caffeic acid (1), chlorogenic acid (2), cryptochlorogenic acid (3), panasenoside (4), and (6R,7E,9R)-4,7-megastigmadien-3-one-9-β-D-glucopyranoside (5). Compounds 3 and 4 were isolated for the first time from the leaves of S. melongena L. in this study.

In cumulative transfer functions, as number of transfer increase, the impact of individual transfer to transfer cost increase linearly or non linearly. This function can effectively explain various passengers`s travel behavior who choose their travel routes in integrated transit line networks including bus and railway modes. Using the function, it is possible to simulate general situations such that even though more travel times are expected, less number of transfer routes are preferred. However, because travel cost with cumulative transfer function is known as non additive cost function types in route search algorithms, finding an optimal route in integrated transit networks is confronted by the insolvable enumeration of all routes in many cases. This research proposes a methodology for finding an optimal path considering cumulative transfer function. For this purpose, the reversal phenomenon of optimal path generated in route search process is explained. Also a heuristic methodology for selecting an optimal route among multiple routes predefined by the K path algorithm. The incoming link based entire path deletion method is adopted for finding K ranking path thanks to the merit of security of route optimality condition. Through case studies the proposed methodology is discussed in terms of the applicability of real situations.

The fruits of Morus alba L. were extracted with 80 % aqueous MeOH, and the concentrated extract was partitioned into EtOAc, n-butyl alcohol, and water fractions. The repeated silica gel () and octadecyl silica gel column chromatographies for the EtOAc and n-butyl alcohol fractions led to isolation of two phenolic compounds. The chemical structures of the compounds were determined as Diels-Alder type adducts, mulberrofuran E (1) and chalcomoracin (2) based on spectroscopic data analyses including nuclear magnetic resonance, mass spectrometry, and infrared spectrometry. Compounds 1 and 2 were isolated for the first time from the fruits of M. alba L. in this study.

Though Dieckol, a phlorotannin of Ecklonia cava, was known to have antioxidant, anticancer, antidiabetic, and anti-inflammatory effects, the underlying antifibrotic mechanism of Dieckol still remains unclear until now. Thus, in the current study, the inhibitory mechanism of Dieckol on liver fibrosis was elucidated mainly in hepatic stellate cells (HSCs). Dieckol exerted cytotoxicity in LX-2, HSC-T6, and HepG2 cells with the reduced fibrosis features of large, spread out, and flattened polygonal shapes in LX-2 cells compared to untreated control. Dieckol attenuated the expression of α-SMA and TGF-β1, increased sub-G1 phase population, and induced caspase-3 activation and cleavages of PARP in HSCs. Furthermore, Dieckol decreased phosphorylation of ERK, p38, AKT, NF-kB, and IkB and activated the microRNA(miR)134 level and JNK phosphorylation in HSCs. Conversely, JNK inhbitor SP600125 reversed the effect of Dieckol on PARP, p-NF-kB, α -SMA, and p-JNK in LX-2 cells. Likewise, miR134 overexpression mimic enhanced phosphorylation of JNK and NF-kB and reduced the expression of α-SMA and PARP cleavage, while miR134 inhibitor reversed the ability of Dieckol to cleave PARP and attenuate the expression of α-SMA in LX-2 cells. Overall, our findings suggest that Dieckol suppresses liver fibrosis via caspase activation and miR134 mediated JNK activation and NF-kB inhibition.

Berberine, a major isoquinoline alkaloid found in medicinal herbs, has been reported to possess anti-inflammatory effects; however, the underlying mechanisms responsible for its actions are poorly understood. In the present study, we investigated the inhibitory effects of berberine and the molecular mechanisms involved in lipopolysaccharide (LPS)-treated RAW 264.7 and THP-1 macrophages and its effects in LPS-induced septic shock in mice. In both macrophage cell types, berberine inhibited the LPS-induced nitric oxide (NO) production and inducible NO synthase (iNOS) protein expression, but it had no effect on iNOS mRNA transcription. Suppression of LPS-induced iNOS protein expression by berberine occurred via a human antigen R (HuR)-mediated reduction of iNOS mRNA stability. Molecular data revealed that the suppression on the LPS-induced HuR binding to iNOS mRNA by berberine was accompanied by a reduction in nucleocytoplasmic HuR shuttling. Pretreatment with berberine reduced LPS-induced iNOS protein expression and the cytoplasmic translocation of HuR in liver tissues and increased the survival rate of mice with LPS-induced endotoxemia. These results show that the suppression of iNOS protein expression by berberine under LPS-induced inflammatory conditions is associated with a reduction in iNOS mRNA stability resulting from inhibition of the cytoplasmic translocation of HuR.

A red pigment produced by Zooshikella ganghwensis, was purified by solvent extraction and fractionation. The pigment was identified to be prodigiosin on the basis of spectroscopic data such as 1H-NMR, 13C-NMR, DEPT, 2D-NMR, IR, and FAB-MS. Prodigiosin inhibited matrix metalloproteinase-1 gene expression and the growth of human cancer cell lines, SK-BR-3, HCT-116, SK-OV-3, HeLa, HepG2, and SK-MEL-5.

The migration of vascular smooth muscle cells (VSMCs) may play a crucial role in the pathogenesis of vascular diseases, such as atherosclerosis and post-angioplasty restenosis. Platelet-derived growth factor (PDGF)-BB is a potent mitogen for VSMCs and plays an important role in the intimal accumulation of VSMCs. Magnobovatol, a new neolignan from the fruits of Magnolia obovata, has been shown to have anticancer properties. However, the effects of magnobovatol on VSMCs are unknown. In the present study, we examined the effects of magnobovatol on the PDGF-BB-induced migration of mouse and human VSMCs, as well as the underlying mechanisms. Magnobovatol significantly inhibited the PDGF-BB-induced migration of mouse and human VSMCs without inducing cell death (as shown by MTT assay and wound healing assay). Additionally, we demonstrated that magnobovatol significantly blocked the PDGF-BB-induced phosphorylation of the PDGF receptor (PDGF-R), Akt and extracellular signal-regulated kinase (ERK)1/2 by inhibiting the activation of the PDGF-BB signaling pathway. Moreover, in both mouse and human VSMCs, magnobovatol inhibited PDGF-induced matrix metalloproteinase (MMP)-2 expression at the mRNA and protein level, as well as the proteolytic activity of MMP-2 (as shown by western blot analysis, RT-PCR, gelatin zymography and ELISA). In addition, the sprout outgrowth formation of aortic rings induced by PDGF-BB was inhibited by magnobovatol (as shown by aortic ring assay). Taken together, our findings indicate that magnobovatol inhibits VSMC migration by decreasing MMP-2 expression through PDGF-R and the ERK1/2 and Akt pathways. Our data may improve the understanding of the anti-atherogenic effects of magnobovatol in VSMCs.

In this study, we aimed to determine whether Sanggenon G, an active compound isolated from the root bark of Morus alba, exhibited enhanced anti-immobility activity with the addition of the α2-antagonist yohimbine in rats subjected to forced swim test (FST)-induced depression. Fluoxetine (a selective serotonin reuptake inhibitor) treatment in rats reduced the immobility time, and pretreatment with yohimbine significantly enhanced the antidepressant-like behavior of fluoxetine at 5, 10 and 20 mg/kg. Similarly, Sanggenon G significantly decreased the immobility time, reducing immobility by a maximum of 43.9 % when treated at a dose of 20 mg/kg. Furthermore, pretreatment with yohimbine significantly enhanced the antidepressant-like behavior of Sanggenon G at 5 and 10 mg/kg. Our findings suggest that the antidepressant-like effect of Sanggenon G could be facilitated by concomitant use of the α2-antagonist. Further studies are needed to evaluate the potential of Sanggenon G as an alternative therapeutic approach for the treatment of depression.

Though arjunic acid, a triterpene isolated from Terminalia arjuna, was known to have antioxidant, antiinflammatory, and cytotoxic effects, its underlying antitumor mechanism still remains unclear so far. Thus, in the present study, the molecular antitumor mechanism of arjunic acid was examined in A549 and H460 non-small cell lung cancer (NSCLC) cells. Arjunic acid exerted cytotoxicity by 3-[4, 5-dimethylthiazol-2-yl]-2, 5-diphenyl tetrazolium bromide (MTT) assay and significantly increased sub-G1 population in A549 and H460 cells by cell cycle analysis. Consistently, arjunic acid cleaved poly (ADP-ribose) polymerase (PARP), activated Bax, and phosphorylation of c-Jun N-terminal kinases (JNK), and also attenuated the expression of pro-caspase-3 and Bcl-2 in A549 and H460 cells. Furthermore, arjunic acid upregulated the expression of endoplasmic reticulum (ER) stress proteins such as IRE1 α, ATF4, p-eIF2α, and C/EBP homologous protein (CHOP) in A549 and H460 cells. Conversely, CHOP depletion attenuated the increase of sub-G1 population by arjunic acid, and also JNK inhibitor SP600125 blocked the cytotoxicity and upregulation of IRE1 α and CHOP induced by arjunic acid in A549 and H460 cells. Overall, our findings suggest that arjunic acid induces apoptosis in NSCLC cells via JNK mediated ER stress pathway as a potent chemotherapeutic agent for NSCLC.

In the present study, the underlying apoptotic mechanism of sanggenol L was elucidated in ovarian cancer cells. Sanggenol L showed cytotoxic and antiproliferative effect in A2780, SKOV-3, and OVCAR-3 ovarian cancer cells in a concentration-dependent fashion. Consistently, sanggenol L increased sub-G1 phase population and early and late apoptotic portion in ovarian cancer cells. Also, sanggenol L activated caspase9/3, suppressed the phosphorylation of IκBα and p65 NF-κB (nuclear factor kappa-light-chain-enhancer of activated B cells), attenuated the expression of Cyclin D1, and cleaved poly(adenosine diphosphate ribose -ribose) polymerase in SKOV-3, A2780, and OVCAR-3 cells. Furthermore, sanggenol L blocked nuclear translocation of NF-κB and also attenuated the expression of NF-κB related genes such as c-Myc, Cyclin D1, and Bcl-X L, Bcl-2, in lipopolysaccharide-treated SKOV-3 cells. Overall, our findings for the first time suggest that sanggenol L induces apoptosis via caspase activation and inhibition of NF-κB/IκBα phosphorylation as a potent chemotherapeutic agent for ovarian cancers.

In this study, an analysis was performed on the performance of the solar water heating system with geo-thermal heat pump for a detached house. This system has a flat plate solar collector (8 m 2 ) and a 3 RT heat pump. The heat pump acts as an auxiliary heater of the solar water heating system. These systems were installed at four individual houses with the same area of 100 m 2 . The monitoring results for one year are as follows. (1) The average daily operating time of the solar system appeared to be 313 minutes in spring (intermediate season), and 135 minutes and 76 minutes in winter and summer respectively. The reason for the short operating time in summer is the high storage temperature due to low water heating load. The high storage temperature is caused by a decrease in collecting efficiency as well as by overheating. (2) The geothermal heat pump as an auxiliary heater mainly operates on days of poor insolation during the winter season. (3) Despite controlling for total house area, hot water consumption varies greatly according to the number of people in the family, hot water usage habits, etc. (4) The yearly solar fraction was 69.8 to 91.5 percent, which exceeds the maximum value of 80% as recommended by ASHRAE. So the solar collector area of 8 m 2 appeared to be somewhat greater for the house with an area of 100 m 2 . (5) The observed annual efficiency of solar systems was relatively low at 13.5 to 23.6%, which was analyzed to be due to the decrease in thermal efficiency and the overheating caused by a high solar fraction.

One new feruloyl sucrose ester, 3-feruloyl-4′,6′-diacetyl sucrose (1), along with five known feruloyl sucrose esters, 3,6-diferuloyl-3′,6′-diacetyl sucrose (2), smilaside A (3), 3,6-diferuloyl-6′-acetyl sucrose (4), 3-feruloyl-6′-acetyl sucrose (5), and 3,6-diferuloyl sucrose (6), was isolated from Oryza sativa roots. The chemical structures of the compounds were determined by spectroscopic data analysis. The six isolated feruloyl sucrose esters were evaluated for their inhibitory effect on mushroom tyrosinase in vitro.

A phytochemical investigation of the whole plants of Adonis multiflora Nishikawa & Koki Ito. resulted in the isolation and identification of two new cardenolides—adonioside A (1) and adonioside B (6)—as well as four known cardenolides: tupichinolide (2) oleandrine (3), cryptostigmin II (4), and cymarin (5). Their structures were elucidated on the basis of NMR, MS, and IR spectroscopic analyses. Compounds 1, 2, 5, and 6 showed significant cytotoxicity against six human cancer cell lines (HCT-116, HepG2, HeLa, SK-OV-3, and SK-MEL-5, and SK-BR-3).

Short-chain fatty acids (SCFAs), especially butyrate, produced in mammalian intestinal tracts via fermentation of dietary fiber, are known biofunctional compounds in humans. However, the variability of fermentable fiber consumed on a daily basis and the diversity of gut microbiota within individuals often limits the production of short-chain fatty acids in the human gut. In this study, we attempted to enhance the butyrate levels in human fecal samples by utilizing butyl-fructooligosaccharides (B-FOS) as a novel prebiotic substance. Two major types of B-FOS (GF3-1B and GF3-2B), composed of short-chain fructooligosaccharides (FOS) bound to one or two butyric groups by ester bonds, were synthesized. Qualitative analysis of these B-FOS using Fourier transform infrared (FT-IR) spectroscopy, matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF-MS), nuclear magnetic resonance (NMR) and low-resolution fast-atom bombardment mass spectra (LR-FAB-MS), showed that the chemical structure of GF3-1B and GF3-2B were [O-(1-buty-&beta, D-fru-(2&rarr, 1)-O-&beta, D-fru-O-&alpha, D-glu] and [O-(1-buty)-&beta, 1)-O-(4-buty)-&beta, D-glu], respectively. The ratio of these two compounds was approximately 5:3. To verify their biofunctionality as prebiotic oligosaccharides, proliferation and survival patterns of human fecal microbiota were examined in vitro via 16S rRNA metagenomics analysis compared to a positive FOS control and a negative control without a carbon source. B-FOS treatment showed different enrichment patterns on the fecal microbiota community during fermentation, and especially stimulated the growth of major butyrate producing bacterial consortia and modulated specific butyrate producing pathways with significantly enhanced butyrate levels. Furthermore, the relative abundance of Fusobacterium and ammonia production with related metabolic genes were greatly reduced with B-FOS and FOS treatment compared to the control group. These findings indicate that B-FOS differentially promotes butyrate production through the enhancement of butyrate-producing bacteria and their metabolic genes, and can be applied as a novel prebiotic compound in vivo.

Background: The fruits of Schisandra chinensis have been used traditionally as the medicinal materials in East Asia. Their extracts have been reported to be cytotoxic to several cancer cells and phytochemical research has identified numerous cytotoxic lignans. Objectives: We reviewed for the effects of cytotoxic lignans against various human cancer cells. Materials and Methods: Solvent extraction of fruits in aqueous methanol and fractionation of the extract into H2O, n-BuOH, and EtOAc fractions (Fr) were carried out. Column chromatography (CC) of the non-polar EtOAc Fr, which indicated cytotoxicity to cancer cells, was performed to isolate the cytotoxic lignin. They were identified on the basis of the intensive spectroscopic interpretation of IR, 1D-, 2D-NMR, and mass spectrometry data. The cytotoxicity was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay and cell staining using Hoechst 32258 and propidium iodide. Results: Anwulignan was isolated and identified as a cytotoxic principal component. The IC50 value was calculated to be 22.01 ± 1.87, 156.04 ± 6.71, and 32.68 ± 2.21 μM for human stomach adenocarcinoma, human colon cancer (HT29), and human cervical cancer cells, respectively. Conclusion: Solvent extraction, systematic fractionation, and repeated CC for S. chinensis fruits led to the isolation of a lignin identified to be anwulignan based on various spectroscopic analyses. Anwulignan demonstrated very high cytotoxicity to most human cancer cell lines, and cell death was induced by apoptosis.

In the food industry and herbal markets, it is critical to control the quality of processed Panax ginseng products. In this study, ultra-performance liquid chromatography coupled to quadrupole time of flight mass spectrometry (UPLC-QTOF/MS)-based metabolomics was applied for the quality evaluation of white ginseng (WG), tae-geuk ginseng (TG), red ginseng (RG), and black ginseng (BG). Diverse metabolites including ginsenosides were profiled by UPLC-QTOF/MS, and the datasets of WG, TG, RG, and BG were then subjected to multivariate analyses. In principal component analysis (PCA), four processed ginseng products were well-differentiated, and several ginsenosides were identified as major components of each product. S-plot also characterized the metabolic changes between two processed ginseng products, and the major ginsenosides of each product were found as follows: WG (M-Rb1, M-Rb2, M-Rc, Re, Rg1), TG (Rb2, Rc, Rd, Re, Rg1), RG (Rb1, Rb2, Rc, Rd, Re, Rg1), and BG (Rd, Rk1, Rg5, Rg3). Furthermore, the quantitative contents of ginsenosides were evaluated from the four processed ginseng products. Finally, it was indicated that the proposed metabolomics approach was useful for the quality evaluation and control of processed ginseng products.

Six lignans including two new lignans were obtained as the principal components of the Forsythia koreana flowers via silica gel (SiO2 ), octadecyl SiO2 (ODS) as well as Sephadex LH-20 column chromatography. In addition to two new lignans, named koreanaside A ((7R,8S,7'R,8'S)-7,7'-diepoxy-5'-hydroxy-3,3'-dimethoxylignan 4-O-β-d-glucopyranoside) and koreanaside B ((7R,8S,7'S,8'R)-7,9'-epoxy-9,5',7'-trihydroxy-3,3'-dimethoxylignan 4-O-β-d-glucopyranoside), four known lignans were identified to be (+)-phylligenin, (-)-epipinoresinol, pinoresinol, and tinosposide A. The structures and absolute configurations of koreanasides A and B were established by means of analysis of spectroscopic data (NMR, IR, FAB-MS, and CD), whereas the structures of known lignans were identified by comparison their NMR and MS values with those in the reported literature. Their chemical structures including configuration were established by means of analysis of spectroscopic data (NMR, IR, FAB-MS, and CD) but also comparison of their NMR and MS values with those in the reported literature. This is the first article for isolation of six lignans of F. koreana flowers. Koreanasides A and B showed high radical scavenging activity with oxygen radical absorbance capacity (ORAC) values of 0.97 ± 0.01 and 1.02 ± 0.01, respectively. Koreanaside A also prohibited expressing VCAM-1 in MOVAS cells with 80.5% at 25 mg/mL.

Desulfurococcus amylolyticus is an anaerobic and hyperthermophilic crenarchaeon that can use various carbohydrates as energy sources. We found a gene encoding a glycoside hydrolase family 57 amylolytic enzymes (DApu) in a putative carbohydrate utilization gene cluster in the genome of D. amylolyticus . This gene has an open reading frame of 1,878 bp and consists of 626 amino acids with a molecular mass of 71 kDa. Recombinant DApu (rDApu) completely hydrolyzed pullulan to maltotriose by attacking α-1,6-glycosidic linkages, and was able to produce glucose and maltose from soluble starch and amylopectin. Although rDApu showed no activity toward α-cyclodextrin (CD) and β-CD, maltooctaose (G8) was detected from reaction with γ-CD. The highest activity of rDApu was measured at pH 5.0 and 95 °C. The half-life of rDApu was 12.7 h at 95 °C and 27 min at 98 °C. Interestingly, rDApu was able to transfer a maltose unit to 6- O -α-maltosyl-β-CD via transglycosylation. Structure analysis using MALDI-TOF/TOF MS and nuclear magnetic resonance revealed that the new transglycosylated products were 6 1 , 6 4 -di- O -maltosyl-β-CD and 6 1 , 6 3 , 6 5 -tri- O -maltosyl-β-CD.

Acanthopanax sessiliflorus (Rupr. & Maxim.) Seem., which belongs to the Araliaceae family, mainly inhabits Korea, China, and Japan. Traditionally, Acanthopanax species have been used as treatment for several diseases such as diabetes, tumors, and rheumatoid arthritis. Especially, its fruits have many biological functions including antitumor, immunostimulating, antithrombosis, and antiplatelet activities. Recently, the extract of A. sessiliflorus fruit has been reported to have antithrombotic and antiplatelet activities related to the alleviation of hypertension. Therefore, we investigated the antihypertensive effect of ethanolic extract from A. sessiliflorus fruits (DHP1501) through in vivo, ex vivo, and in vitro studies. In this study, DHP1501 demonstrated free radical scavenging capacity, enhanced endothelial nitric oxide (NO) production, and inhibited angiotensin-converting enzyme (ACE) activity in spontaneously hypertensive rats (SHRs), resulting in the improvement of vascular relaxation and decrease in blood pressure in the hypertensive animal model. These results suggest that A. sessiliflorus fruit extract may be a promising functional material for the prevention and treatment of hypertension. Furthermore, this study demonstrated the utility of MS-based active compounds for the quality control of DHP1501.

α-Flavone glycosides have beneficial properties for applications in the pharmaceutical, cosmetic, and food industries. However, their chemical syntheses are often limited by a low efficiency or scarcity of substrates. In this study, α-flavone glucosides were enzymatically synthesized by amylosucrase from Deinococcus geothermalis (DGAS) using sucrose and various flavones as a donor for glucosyl units and acceptors, respectively. Luteolin was the most effective acceptor in the transglucosylation reaction using DGAS among nine flavone materials (apigenin, chrysin, 6,7-dihydroxyflavone, homoorientin, 7-hydroxyflavone, isorhoifolin, luteolin, luteolin-3',7-diglucoside, and orientin). The highest production yield of luteolin glucoside was 86%, with a 7:1 molar ratio of donor to acceptor molecules, in 50 mM Tris-HCl buffer (pH 7) at 37°C for 24 h using 2 U of DGAS. The synthesized luteolin glucoside was identified as luteolin-4'-O-α-D-glucopyranoside with a glucose molecule linked to the C-4' position on the B-ring of luteolin via an α-glucosidic bond, as determined by 1H and 13C nuclear magnetic resonance. This result clearly confirmed that the glucosylated luteolin was successfully synthesized by DGAS and it can be applied as a functional ingredient. Furthermore, this approach using DGAS has the potential to be utilized for the synthesis of various glucosylated products using different types of polyphenols to enhance their functionalities.

Cachexia and sarcopenia are the main causes of muscle atrophy. These result in a reduction in the muscle fiber area, myo-protein content, and muscle strength, with various molecular modulators being involved. Although several reports have proposed potential therapeutic agents, no effective treatments have been found for muscle atrophy. We searched for myogenic modulators from medicinal plants to treat muscle diseases. We isolated six alkaloids from Corydalis turtschaninovii and evaluated their myogenic potential by using the MyoD reporter gene assay in C2C12 cells. Among the tested compounds, canadine showed the strongest transactivation of MyoD and increased MHC expression during myogenesis. The activation of p38 MAP kinase and Akt are major mechanisms that contribute to the myogenesis by canadine. Canadine increased the number of multinucleated and cylinder-shaped myotubes during myogenesis of C2C12 myoblasts. To determine the preventive effect of canadine in cancer-induced muscle wasting, differentiated C2C12 myotubes were treated with conditioned media from CT26 colon carcinoma culture (CT26 CM) in the presence of canadine. Canadine ameliorated the muscle protein degradation caused by CT26-CM by down-regulating the muscle specific-E3 ligases, MAFbx/atrogin-1 and MuRF1. In this study, we found that canadine from C. turtschaninovii stimulates myogenesis and also inhibits muscle protein degradation. Therefore, we suggest canadine as a protective agent against muscle atrophy.

Investigation of phytochemicals from Magnolia obovata fruit led to the isolation of three novel phenylpropanoid glycosides: obovatoside A-C (1-3) and two known phenylpropanoids, syringin (4) and pavonisol (5). The structures of 1-5 were determined by NMR, HRMS, IR and CD spectroscopic analyses. All compounds were evaluated for their effects on recovery from alloxan-induced pancreatic islet damage in zebrafish. All compounds increased the size of the injured pancreatic islet from 0.60- to 1.14-fold. Compounds 1 and 3-5 significantly increased glucose absorption in zebrafish.

The flowers of Chionanthus retusus Lindl. & Paxton were extracted with 80% aqueous MeOH at room temperature. The concentrated extract was partitioned as EtOAc, n-BuOH, and H2O fractions. From the EtOAc fraction, two triterpenoids and two sterols were isolated using the repeated silica gel (SiO2) and octadecyl SiO2 (ODS) column chromatographies. According to the results of physico-chemical and spectroscopic data including nuclear magnetic resonance, mass spectrometry, and infrared. The chemical structures of the compounds were respectively determined as ursolic acid (1), corosolic acid (2), β-sitosterol (3), and daucosterol (4). All the compounds were isolated for the first time from the flowers of Chionanthus retusus Lindl. & Paxton.

A new pregnane hexaglycoside, named amurensioside L (1), was isolated from the whole plant of Adonis multiflora. Amurensioside L (1) emerged to be new pregnane hexaglycoside which we fully spectroscopically characterized. The chemical structure of compound 1 was established as 14β,20R-epoxy-3β-hydroxypregna-4,6-dien-18-oic acid-20-lactone 3-O-β-d-glucopyranosyl-(1 → 4)-O-β-d-diginopyranosyl-(1 → 4)-O-β-d-cymaropyranosyl-(1 → 4)-O-β-d-cymaropyranosyl-(1 → 4)-O-β-d-oleandropyranosyl-(1 → 4)-O-β-d-oleandropyranoside on the basis of spectroscopic analyses including nuclear magnetic resonance spectrometry, high-resolution fast atom bombardment mass spectrometry, and infrared spectroscopy.

One new phenylglycoside, 1-hydroxy-3,4,5-trimethoxyphenyl-1-O-[6′-O-(4″-carboxy-1″ ,3″ ,5″ - trihydroxy)phenyl]-β-D-glucopyranoside (1), along with eight known ones, isosalicin (2), vanilloloside (3), (4-hydroxy-3,5-dimethoxyphenyl)methyl-β-D-glucopyranoside (4), crenatin (5), hydrageifolin I (6), tachioside (7), isotachioside (8), and koaburside (9), were isolated from the stems of Spiraea prunifolia var. simpliciflora. The chemical structures of these compounds were identified on the basis of spectroscopic data such as NMR, FAB-MS, and IR. All these compounds were isolated from this plant for the first time.

The calyx of Fragaria ananassa (Rosaceae) has not been investigated for its chemical constituents and biological activity. This study focused on the isolation of active metabolites from the calyx of this plant. Compounds from F. ananassa calyx were extracted in 80 % aqueous MeOH and the concentrated extract was successively partitioned into EtOAc, n-BuOH, and H2O fractions. Repeated silica gel, octadecyl silica gel, and Sephadex LH-20 column chromatographies afforded six purified flavonoids. On the basis of spectroscopic methods, including 1H, 13C nuclear magnetic resonance spectrometry (NMR), DEPT, and 2D NMR (gCOSY, gHSQC, gHMBC), the flavonoids were identified as kaempferol (1), astragalin (2), quercetin (3), isoquercitrin (4), sexangularetin (5), and sinensin (6). All the flavonoids were isolated for the first time from the F. ananassa calyx in this study. The flavonoids were evaluated for radical-scavenging capacity 2,2′-azinobis (3-ethylbenzothiazoline-6-sulfonic acid ammonium salt), 2,2-diphenyl-1-picrylhydrazyl, and oxygen radical absorbance capacity methods. In conclusion, quercetin (3) consistently showed the highest ABTS, DPPH, and ORAC radical-scavenging activities compared with the other isolated flavonoids.

This study analyzed analyzes the energy performance of six houses in Daejeon completed which were built in 2011. Observed The observed houses, which were all designed and constructed inof the same size and structure, are were highly insulated with triple Low-E coating windows; the insulation level of the walls is was 0.13 W/㎡K and that of the roof is was 0.10 W/㎡K. As electric houses, all of the energy supplied to the houses, including for cooking, is was supplied by electricity. A and 3~4 kWp of photovoltaic system and a 3~5 kW of ground source heat pump (GSHP) were installed in each house tofor providing provide space heating/and cooling and hot water are installed. We constructed a Web-based remote monitoring system in order to understand energy consumption and the dynamic behavior of the energy system. T, and the results of our metering data analysis of 2013 are as follows. First, the annual residential energy consumption is was 4,400 kWh (σ = 1,209) and GSHP energy consumption is was 5,182 kWh (σ = 1,164). Second, residential energy consumption ranked highest in average energy usage, with at 45% of the total, followed by heating with at 30%, hot water supply with at 17% and cooling with at 6%. Third, the average energy independence rate is was 51.8%, the GFA (Gross gross floor area) criteria average energy consumption unit is was 48.7 kWh/㎡yr (σ = 10.1), and the net energy consumption unit (except the energy yield of the PV systems) is was 24.7 kWh/㎡yr (σ = 8.8).

Chromatographic methods such as silica gel, ODS, and Sephadex LH-20 column chromatographic techniques were used to identify three new phenylethanoid glycosides along with three known ones, 2-(3,4-dihydroxyphenyl)ethyl o-α-L-rhamnopyranosyl-(1→2)-β-D-allopyranoside (1), magnoloside D (2), and magnoloside A (3), from the fruits of Magnolia obovata. Using the spectroscopic data, including NMR, MS, and IR, the new phenylethanoid glycosides were identified and named magnoloside F (4), magnoloside G (5), and magnoloside H (6).

Fruits of Rhus parviflora were extracted with 80% aqueous methanol (MeOH), and the concentrated extract was partitioned using ethyl acetate (EtOAc), n-butanol (n-BuOH), and H2O, successively. Purification of EtOAc fraction led to isolation of fifteen polyphenols of which structures were identified by spectroscopic methods including 2D-NMR. Most compounds apart from compound 10 inhibited low density lipoprotein- oxidation within IC50 value of 10 µM. Among compounds, taxifolin (2), quercetin 3-O-α-L-rhamnopyranoside (13), agathisflavone (5) sulfuretin (4), and aureusidin (3) showed IC50 values 0.9, 0.8, 5.8, 2.9, and 2.4 µM which were of highly significant in comparison positive control butylated hydroxytoluene with IC50 value of 2.1 µM. The results indicate fruits of R. parviflora as a source of anti- hypercholesterolemic compounds.

This study was designed to investigate the antitumor mechanism of Phytol in hepatocellular carcinomas including Huh7 and HepG2 cells in association with caspase dependent apoptosis and epithelial mesenchymal transition (EMT) signaling. Phytol significantly suppressed the viability of Huh7 and HepG2 cells. Also, Phytol significantly increased the sub G1 population and terminal deoxynucleotidyl transferase deoxyuridine triphosphate nick end labeling (TUNEL) positive cells in a concentration dependent manner in Huh7 and HepG2 cells. Consistently, Phytol cleaved poly (adenosine diphosphate-ribose) polymerase (PARP), activated caspase-9/3, and Bax attenuated the expression of survival genes such as Bcl-2, Mcl-1, and c-Myc in Huh7 and HepG2 cells. Of note, Phytol also suppressed typical morphology change of EMT such as loss of cell adhesion and formation of fibroblast like mesenchymal cells in HepG2 cells. Furthermore, Phytol also reversed the loss of E-cadherin and overexpression of p-smad2/3, alpha-smooth muscle actin, and Snail induced by EMT promoter transforming growth factor beta1 in HepG2 cells. Overall, our findings suggest that Phytol exerts antitumor activity via apoptosis induction through activation of caspas-9/3 and inhibition of EMT in hepatocellular carcinoma cells as a potent anticancer candidate for liver cancer treatment.