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Lindera erythrocarpa contains various constituents such as cyclopentenedione-, flavonoid-, and chalcone-type components. In this study, a novel bi-linderone derivative and 17 known compounds were isolated from the leaves of L. erythrocarpa by using various chromatographic methods. The structures of the components were determined from nuclear magnetic resonance and mass spectrometry data. All isolated compounds were tested for anti-inflammatory and anti-neuroinflammatory activities in lipopolysaccharide (LPS)-induced BV2 and RAW264.7 cells. Some of these compounds showed anti-inflammatory effects by inhibiting the nitric oxide (NO) produced by LPS. In particular, linderaspirone A (16), bi-linderone (17) and novel compound demethoxy-bi-linderone (18) showed significant inhibitory effects on the production of prostaglandin E2 (PGE2), tumor necrosis factor-α, and interleukin-6. The three compounds also inhibited the expression of inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2), which are pro-inflammatory proteins, and the activation of nuclear factor κB (NF-κB). Therefore, linderaspirone A (16), bi-linderone (17), and demethoxy-bi-linderone (18) isolated from the leaves of L. erythrocarpa have therapeutic potential in neuroinflammatory diseases.

Linderone is a major compound in Lindera erythrocarpa and exhibits anti-inflammatory effects in BV2 cells. This study investigated the neuroprotective effects and mechanisms of linderone action in BV2 and HT22 cells. Linderone suppressed lipopolysaccharide (LPS)-induced inducible nitric oxide synthase, cyclooxygenase-2, and pro-inflammatory cytokines (e.g., tumor necrosis factor alpha, interleukin-6, and prostaglandin E-2) in BV2 cells. Linderone treatment also inhibited the LPS-induced activation of p65 nuclear factor-kappa B, protecting against oxidative stress in glutamate-stimulated HT22 cells. Furthermore, linderone activated the translocation of nuclear factor E2-related factor 2 and induces the expression of heme oxygenase-1. These findings provided a mechanistic explanation of the antioxidant and anti-neuroinflammatory effects of linderone. In conclusion, our study demonstrated the therapeutic potential of linderone in neuronal diseases.

The ethyl acetate fraction obtained from aerial parts of L. lucidus was subjected for isolation of new bioactive compounds, which enabled isolation of five new pimarane-type diterpenoids, namely, 3β, 8β, 12β, 18-tetrahydroxy pimar-15-ene (10), 7α, 8β, 12β, 18-tetrahydroxy pimar-15-ene (11), 3β, 8β, 11β, 12α, 18-pentahydroxy pimar-15-ene (12), 12β acetoxy, 8β, 3β, 18-trihydroxy pimar-15-ene (13), and 3β acetoxy, 8β, 12β, 18-trihydroxy pimar-15-ene (14), along with nine known compounds. The structures were elucidated by spectroscopic analysis and comparison with literature data. The isolated new pimarane diterpenoids were examined for antimicrobial activity against Gram-negative and Gram-positive bacteria strains. Among them, the compound 3β, 8β, 12β, 18-tetrahydroxy pimar-15-ene (10) was most effective, exhibiting minimum inhibitory concentration (MIC) values of 15.62 µg/mL against Staphylococcus epidermidis, 31.25 µg/mL against Staphylococcus aureus, 62.5 µg/mL against Pseudomonas aeruginosa, and 125 µg/mL against Escherichia coli.

Obesity is a life-threatening metabolic disorder necessitating urgent development of safe and effective therapy. Currently, limited such therapeutic measures are available for obesity. The present study was designed to develop a novel, safe and effective herbal therapy for the management of obesity. A polyherbal formulation (18KHT01) was developed by homogeneously mixing a specific proportion of crude Quercus acutissima (acorn jelly powder), Camellia sinensis (dry leaf buds), and Geranium thunbergii (dry aerial part) along with Citrus limon (fruit juice). Synergistic antioxidant, antiadipogenic, and anti-obesity activities were evaluated by in vitro as well as in vivo studies. In vitro experiments revealed strong synergistic antioxidant and anti-adipogenic activities of 18KHT01. Molecular assessment of 18KHT01 showed significant down-regulation of vital adipogenic factors such as PPARγ, C/EBPα, aP2, SREBP-1c, FAS, and LPL. Based on the results of the preliminary toxicity study, 75 and 150 mg/kg, twice daily doses of 18KHT01 were administered to evaluate anti-obesity activity in diet-induced obese (DIO) C57BL/6J mice model. The major obesity-related parameters such as body weight, weight gain, food efficiency ratio, as well as serum lipid profile were significantly reduced by 18KHT01 with potential synergism. Also, the high-fat diet-induced insulin resistance was suggestively alleviated by the formulation, and thus ameliorated fasting blood glucose. Histological evaluation of liver and white adipose tissue revealed that the significant reduction of fat depositions and thus reduction of these tissue weights. Synergy evaluation experiments exhibited that the 18KHT01 offered strong synergism by improving efficacy and reducing the toxicity of its ingredients. Overall results evidenced the 18KHT01 as a safe and potent anti-obesity herbal therapy.

Acanthopanax trifoliatus (L.) Merr. have been used as folk medicine to treat various diseases traditionally and the young leaves and shoots of A. trifoliatus are popularly consumed as vegetables and herbal tea in southern China. In the study, we firstly tested the cytotoxicity and NO production of 18 fractions that extracted from the leaves, stems and roots of A. trifoliatus to select the bioactive fraction. The increasing evidence suggested that the dichloromethane extract prepared from stems of A. trifoliatus (ATSDC) have anti-inflammatory activity. Therefore, the study followed to investigate the effects of ATSDC on the inflammatory response and the molecular mechanisms underpinning this effect in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. The manuscript showed that ATSDC effectively inhibited NO production in LPS-stimulated cells and significantly reduced the production of pro-inflammatory cytokines IL-6, at a dose of 40 µg/mL, whereas TNF-α production tended to decrease under ATSDC treatment. We also confirmed a dose-dependent and significant inhibition of iNOS and COX-2 protein expression. In conclusion, ATSDC exerted strong inhibitory effect on the expression of iNOS and COX-2 protein in LPS-induced RAW 264.7 macrophages and could be potentially used in treatment of inflammatory-related diseases in the future.

The ethyl acetate fraction obtained from aerial parts of

현대사회에서 회사는 경제활동의 주체로서 중추적 역할을 담당하고 있으며, 회사에 관한 규범인 회사법은 기업의 조직과 운영은 물론 국민경제에 중대한 영향을 미친다. 따라서 기업을 활성화하고 국가의 경쟁력을 향상시키기 위하여는 회사법제를 쉽게 이해할 수 있고 급변하는 경제환경에 신속하게 대응할 수 있도록 구축하여야 한다. 우리 회사법은 1962년에 제정된 상법 중 제3편에 규정되어 있으나, 상법의 각 편에 공통된 법원리가 지배하고 있는 것은 아니다. 특히, 회사편은 다른 편들과는 달리 전통적으로 단체법적 성질을 반영한 강행법적 규정들로 이루어져 있다. 따라서 상법의 각 편들을 반드시 하나의 법전에 포함시켜야 할 이유는 없다. 외국의 입법례를 보면, 우리 상법 제정 시에 모범으로 삼은 국가인 독일은 이미 1937년에 상법전에서 주식회사와 주식합자회사에 관한 규정을 분리하여 주식법을 단행법으로 제정하였고, 일본도 2005년에 기존의 상법에서 회사편을 분리하여 회사법을 단행법으로 제정하였다. 판례법 국가인 영국과 미국에서도 일찍이 회사법을 단행법으로 제정하였다. 그러므로 우리 회사법도 글로벌스탠더드에 맞추어 단행법화하고 법률규정을 체계적으로 통합·정비할 필요가 있다. 현행 회사에 관한 규범은 상법 제정 이후 여러 차례의 회사편 개정이 이루어지면서 상호충돌되는 규정들이 존재하고 회사편과 각 법률에 산재되어 있는 회사관련 규정들 사이에서도 법체계의 부조화와 상호충돌 문제가 발생하고 있다. 회사법을 단행법으로 입법하는 경우에 모든 회사를 규율하는 통합법의 형태를 갖출 필요가 있다. 회사법이 이용자 또는 수요자 중심의 체계를 갖추기 위하여는 가장 많이 이용되고 있는 주식회사를 중심으로 규정하고, 주식회사 중에서도 비상장주식회사를 기본으로 삼아 규정하여야 할 것이다. 단행법으로서의 회사법은 회사의 설립, 조직, 운영, 관리에 관한 것을 완결적이며 각 규정 간에 정합성을 확보할 수 있는 방향으로 규율하는 체계로 구축되어야 한다. 특히, 상장회사의 특례규정을 상법(지배구조에 관한 규정)과 자본시장법(재무관리에 관한 규정)에 분리하여 규정함으로써 발생한 법체계의 문제점을 해소하여야 한다. 이를 위하여 단행법으로 제정하는 회사법에서는 회사에 관한 특례를 가능한 한 모두 포섭하여 규정할 필요가 있다. 자본시장법상의 상장회사에 대한 특례는 법역의 정합성 측면에서도 회사법으로 옮기는 것이 바람직하다. 상장회사에 대한 특례는 한 곳에 모아 규정하는 것보다는 개별적으로 일반규정 다음에 특례규정을 두는 것이 수범자가 회사법의 규율내용을 쉽게 이해할 수 있다. 회사법의 규정은 수범자의 관점에서 명확하고 체계적이어야 한다. 입법기술상의 편리성과 법률의 간결성보다 수범자의 편리성, 규율내용에 대한 이해의 수월성 및 법규 준수가능성의 제고를 우선하여야 한다. 준용규정은 입법기술상의 편리성으로 유사한 내용의 중복을 피하고 조항 수를 감소시켜 법률의 간결성을 확보하는 장점이 있으나, 수범자의 편의성을 크게 해치는 단점이 있으며, 개정 과정에서 입법상 오류를 초래하는 경우도 있다. 따라서 수범자의 편의성을 확보하기 위해서는 준용규정을 최소화하여야 한다. 그 밖에 상법은 회사와 관련된 벌칙을 제3편 제7장에서 일괄하여 규정하고 있다. 그러나 이러한 입법방식은 수범자의 입장에서 그 내용을 찾는 데 어려움을 주고 위반행위에 대한 벌칙을 제대로 이해하지 못할 가능성이 높다. 따라서 수범자가 준수하여야 할 사항을 규정하고 해당 조항에서 그 위반행위에 대한 벌칙을 규정하는 것이 바람직하다.

Power Beacons (PBs) can transfer energy wirelessly to devices in a wireless powered communication network. When PBs are deployed in an IEEE 802.11 Wireless LAN (WLAN), the energy transfer of PBs may interfere with the Wi-Fi stations if Wi-Fi stations and PBs share the same frequency band. In this letter, to resolve this interference problem, we propose a new Medium Access Control (MAC) protocol for IEEE 802.11 Wi-Fi stations to efficiently coexist with PBs. PBs contend just as Wi-Fi stations to gain opportunity for transferring energy and determine its operation based on the average energy level of stations. It is demonstrated that the throughput of the proposed MAC protocol is superior to that of IEEE 802.11 WLAN without interference control.

Five known flavonoid glycosides namely, juglanin (1), astragalin (2), nicotiflorin (3), isoquercetin (4) and apigenin-7-O- b -glucuronide (5), and a phenolic glucoside, arbutin (6), were isolated for the first time from the leaves of Afgekia mahidolae (Fabaceae). Their structures were elucidated using one- and two-dimensional NMR spectroscopic methods and comparison with the literature. The ability of 1-4 to promote the migration of CCD-1064sk fibroblasts into a scratch-wound area was evaluated. The results indicated that juglanin (1) and nicotiflorin (3) significantly increased the migration of these cells and, hence, supporting the wound healing effect of flavonol glycosides.

A phytochemical investigation into the bark of Erythrophleum fordii yielded four new compounds, two new cassaine diterpenoids (erythrofordin T and U, 1 and 2) and two new cassaine diterpenoid amines (erythroformine A and B, 6 and 7), as well as nine known compounds. We report for the first time the isolation of erythrofordin V (3) from a natural source and that of the remaining eight known diterpenoids (4-5, 8-13) from E. fordii. All structures were elucidated using spectroscopic analysis. Cytotoxic activity of the isolated compounds (1-13) was examined in vitro against three non-small cell lung cancer cell lines (A549, NCI-H1975, and NCI-H1229) using the MTT assay. Cassaine diterpene amines (6-10, 12, 13) exhibited potent cytotoxic activity against all three cell lines with IC50 values between 0.4μM and 5.9μM. Erythroformine B (7) significantly induced apoptosis in all three cancer cells in a concentration-dependent manner.

Background Royal jelly (RJ) has been used traditionally for dietary, cosmetic and health purposes for a long time in different parts of the world. Scientific studies have also shown its numerous health-promoting properties including hypoglycemic and anti-hypercholesterolemic action. In this study, we investigated the anti-adipogenic activity of RJ in 3 T3-L1 cells and isolated the major responsible root component for the activity. Methods An active anti-adipogenic compound was isolated through bioassay-guided isolation process by successive treatment of RJ and its active fractions on 3 T3-L1 cell line. (E)-10-Hydroxy-2-decenoic Acid (10-HDA) was identified using NMR spectroscopy and ultra-performance liquid chromatography (UPLC). As 10-HDA showed significant anti-adipogenic activity with Oil Red O staining and TG content assay on 3 T3-L1 adipocytes, further study was carried out in molecular level for the expression of adipogenic transcription factors such as PPARγ, FABP4, C/EBPα, SREBP-1c, and Leptin. The effect of 10-HDA on preliminary molecules such as pAkt, pERK, C/EBPβ, and pCREB were studied in the early stage of adipogenesis. The effect of 10-HDA on reactive oxygen species (ROS) production in fully differentiating adipocytes was measured by nitro blue tetrazolium (NBT) assay. Result Results showed that triacylglycerol accumulation and ROS production was markedly suppressed by 10-HDA. Preliminary molecules such as pAkt, pERK, pCERB, and C/EBPβ were found to be down-regulated by 10-HDA, which led to down-regulation of key adipogenic transcription factors such as PPARγ, FABP4, CEBPα, SREBP-1c, and Leptin on 3 T3-L1 adipocytes. Conclusion Our results suggest that anti-adipogenesis of 10-HDA on 3 T3-L1 adipocyte takes place via two mechanisms: inhibition of cAMP/PKA pathway and inhibition of p-Akt and MAPK dependent insulin signaling pathway. So it is considered that 10-HDA, a major component of RJ, can be a potential therapeutic medicine for obesity. Electronic supplementary material The online version of this article (10.1186/s12906-018-2423-2) contains supplementary material, which is available to authorized users.

Data on identification and purity assessment of isolated 10-Hydroxy-2-decenoic acid (10-HDA). Figure S1. 1H NMR Spectrum (A) and 13C NMR (500 MHz) spectra (B) of the compound isolated from ethyl acetate fraction of RJ in DMSO-d6; Figure S2. TLC analysis of Royal jelly (RJ), RJ-EA fraction (EA), isolated 10-HDA compound (Com) and standard 10-HDA (Std); Figure S3. Mass spectrometry - structure of the 10-Hydroxy-2-decenoic acid (10-HDA). (DOCX 156 kb)

Triterpenoid saponins are difficult to analyze using high-performance liquid chromatography coupled to UV/vis spectrophotometry due to their lack of chromophores. This study describes the first analytical method for the determination of 15 triterpenoid saponins from the leaves, stems, root bark, and fruits of Acanthopanax henryi, using a high-performance liquid chromatography with charged aerosol detection coupled with electrospray ionization mass spectrometry method. The separation was carried out on a Kinetex XB-C18 column with an acetonitrile/water gradient as the mobile phase, followed by charged aerosol detection. The operating conditions of charged aerosol detection were set at 24 kPa for nitrogen pressure and 100 pA for the detection range. Liquid chromatography with electrospray ionization mass spectrometry is described for the identification of compounds in plant samples. The electrospray ionization mass spectrometry method involved the use of the [M + Na](+) and [M + NH4 ](+) ions for compounds 1-15 in the positive ion mode with an extracted ion chromatogram. The developed method was fully validated in terms of linearity, sensitivity, precision, repeatability, and recovery, then subsequently applied to evaluate the quality of A. henryi.

Three new phenylacylphenol derivatives, stewartianol (1), deoxystewartianol-4'-O-arabinoglucoside (2), and stewartianol-3-O-glucoside (3), along with nine known compounds, methylesculin (4), fraxoside (5), fraxetin (6), scopletin (7), (+)-dihydromyricetin (8), (+)-taxifolin-7-O-β-D-glucose (9), (+)-taxifolin (10), (+)-dihydrokaempferol-7-O-β-D-glucose (11), and 3-acetyl-ursolic acid (12), were isolated from the twigs of Stewartia pseudocamellia; commonly used as folk medicine in Korea. The structures of the isolated compounds were identified using spectroscopic analysis, including 1D, 2D NMR, MS and compared with published data. The compounds were tested for their anti-melanogenic activity in cultured murine B16 melanoma cells. Stewartianol (1) and stewartianol-3-O-glucoside (3) showed an inhibitory effect significantly on melanogenesis in a concentration-dependent manner.

The metabolite changes in Korean mistletoe, as functional food, and their effects on its biological activity were monitored. The Korean mistletoe species were successfully distinguished by hierarchical clustering analysis (HCA) in atmospheric-pressure chemical ionization (APCI) and electrospray ionization (ESI) mode. As shown by the PCA scatter plot and loading plot, the Santalaceae family exhibited significant markers derived from oleanolic acid, whereas the Loranthaceae family exhibited tentative markers derived from glycosidic derivatives of quercetin and kaempferol. The mistletoe extracts also inhibited plasminogen activator inhibitor 1 (PAI-1) differently depending on the mistletoe family. The Santalaceae family was shown to be a potent inhibitor of PAI-1, with an IC 50 value of around 40.0 µg/mL. In contrast, the Loranthaceae family extracts did not inhibit PAI-1. Importantly, discrimination was shown across the chemotaxonomy of the plant, which correlated strongly with the oleanolic acid contents in Korean mistletoe.

Euphorbia supina has been traditionally used for the treatment of furuncle and bloody diarrhea relevant to the inflammatory process. It has been proven to have a variety of pharmacological efficacies including antiarthritic, detoxification, hemostatic, and diuretic activities. RAW 264.7 macrophages and bone marrow-derived mast cells (BMMCs) were used to determine the anti-inflammatory and anti-allergic effects of E. supina (ES). NO production was assayed by measuring the nitrite content of the supernatants of cultured RAW 264.7 cells. β-hexosaminidase, a marker of mast cell degranulation, was quantitated by spectrophotometric analysis. ELISA was used for the analysis of interleukin-6 expression, and Western blotting was used to analyze 5-LOX, iNOS, and MAPK activation. The relevant gene expression upon ES treatment was measured by RT-PCR. ES inhibited inducible nitric oxide synthase (iNOS) in RAW 264.7 cells, and IL-6 and LTC4 production in PMA- and A23187-induced BMMCs along with the downregulation of 5-LOX gene expression. Furthermore, in the present study, a decrease in p-ERK, p-JNK, and p-P38 expression, as well as the suppression of degranulation, were observed by treatment with ES. Further in vivo study revealed that ES treatment also remarkably inhibited xylene-induced mouse ear edema and MPO levels in mice ears. This study demonstrates that ES has a potential regulatory effect on the expression of inflammatory mediators through the inhibition of both the phosphorylation of MAPK signaling and the activation of degranulation.

The increase in inflammatory cytokines and chemokines is a common denominator in the pathogenesis of acute lung injury (ALI) which are involved in the influx of inflammatory cells and lung damage. The aim of the present study was to evaluate the protective effect of 3,4,5-trihydroxycinnamic acid (THC) in lipopolysaccharide (LPS)-induced ALI. THC efficiently decreased the mRNA expression of interleukin-8 (IL-8) in LPS-stimulated A549 airway epithelial cells. THC induced heme oxygenase-1 (HO-1) expression in A549 cells. THC also increased the activation of AMP-activated protein kinase (AMPK) in A549 cells and RAW264.7 macrophages. In LPS-induced ALI in mice, THC significantly suppressed neutrophil influx and monocyte chemoattractant protein-1 (MCP-1) production in the bronchoalveolar lavage fluid (BALF). THC also attenuated the levels of neutrophil elastase (NE), tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) in the BALF and serum. In addition, THC inhibited the expressions of inducible nitric oxide synthase (iNOS) and the activation of nuclear factor-kappa B (NF-κB) in the lung. These protective effects of THC were accompanied with HO-1 induction and AMPK activation. Taken together, the present study clearly demonstrates that THC significantly attenuates the LPS-induced ALI, suggesting that THC might be a valuable therapeutic adjuvant in airway inflammatory disorders.

Sophorae Radix (Sophora flavescens Aiton) has long been used in traditional medicine in East Asia due to the various biological activities of its secondary metabolites. Endogenous contents of phenolic compounds (phenolic acid, flavonol, and isoflavone) and the main bioactive compounds of Sophorae Radix were analyzed based on the qualitative HPLC analysis and evaluated in different organs and at different developmental stages. In total, 11 compounds were detected, and the composition of the roots and aerial parts (leaves, stems, and flowers) was significantly different. trans-Cinnamic acid and p-coumaric acid were observed only in the aerial parts. Large amounts of rutin and maackiain were detected in the roots. Four phenolic acid compounds (benzoic acid, caffeic acid, ferulic acid, and chlorogenic acid) and four flavonol compounds (kaempferol, catechin hydrate, epicatechin, and rutin) were higher in aerial parts than in roots. To identify putative genes involved in phenolic compounds biosynthesis, a total of 41 transcripts were investigated. Expression patterns of these selected genes, as well as the multiple isoforms for the genes, varied by organ and developmental stage, implying that they are involved in the biosynthesis of various phenolic compounds both spatially and temporally.

Two new benzofurans, 2-(3,4-dimethoxyphenyl)-5-(1,3-dihydroxypropyl)-7-methoxybenzofuran (1) and 2-(3,4-methylenedioxyphenyl)-5-(3-hydroxymethyletoxy-1-hydroxypropyl)-7-methoxybenzofuran (2), a new triterpene, 3β, 6β, 21β-trihydroxyolean-12-ene (3), and eleven known compounds were isolated from the stem bark of Styrax obassia. The structures of the isolated compounds were established by extensive spectroscopic analyses, including 1D and 2D NMR and HRMS. Their anti-inflammatory activities were evaluated against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW264.7 macrophages. Compound 1 was shown to reduce LPS-induced iNOS expression in a dose-dependent manner. In addition, pretreating cells with 1 significantly suppressed their LPS-induced expression of COX-2 protein.

Ethnopharmacological relevance Pseudolysimachion rotundum var. subintegrum (Speedwell, Plantaginaceae) is used as a traditional herbal medicine for treating bronchitis, cough and asthma in Korea, China, Russia, and Europe. Aim of the study In this study, we investigated the protective effects of the novel iridoid glycoside, piscroside C (compound 1) isolated from the methanolic extract of P. rotundum var. subintegrum against inflammatory responses using a cigarette smoke induced chronic obstructive pulmonary disease (COPD) and TNF-α-stimulated human airway epithelial NCI-H292 cells. Materials and methods The novel iridoid glycoside piscroside C was isolated from the methanolic extract of P. rotundum var. subintegrum. The chemical structure was established by NMR, HRESIMS, and optical rotation. In in vivo experiment, the mice received 1 h of cigarette smoke for 3 days. Piscroside C was administered to mice by oral gavage 1 h before cigarette smoke exposure for 3 days. In in vitro experiment, we evaluated the effect of piscroside C on proinflammatory mediators in H292 cells stimulated with TNF-α. Results Piscroside C significantly reduced the neutrophil influx, reactive oxygen species production, IL-6, TNF-α, and elastase activity in bronchoalveolar lavage fluid in COPD animals. In addition, piscroside C attenuated NF-κB and IκB phosphorylation, leading to reduced recruitment of inflammatory cells into the lung tissue. Consistent with the results of in vivo experiment, piscroside C significantly inhibited the expression of inflammatory cytokines (IL-6, IL-8 and IL-1β) by inhibiting NF-κB activation, as resulting decrease in the phosphorylation of IKKβ, IκBα and TAK1 in TNF-α-stimulated H292 cells. Conclusion These findings indicate that piscroside C effectively inhibits inflammatory responses, which is an important process in the development of COPD through suppression of IKK/NF-κB activation. Our study suggest that piscroside C might represent a useful therapeutic for the treatment of inflammatory airway disease.

Three new triterpene glycosides (Lonicerosides K, L and M) and 11 known compounds were isolated from the aerial parts of Weigela subsessilis. Among the known isolated compounds, loniceroside A, sweroside, kaempferol-3-O-glucopyranoside 6″-(3-hydroxy-3-methylglutarate), kaempferol-3-O-acetylglucoside and grandifloroside were reported for the first time in a Weigela genus plant. Their chemical structures were identified using extensive spectroscopic analysis including two-dimensional (2D)-NMR experiments, HR-ESI-QTOF-MS and comparison with reported data. Among these compounds, lonicerosides A and L had potent melanogenesis stimulatory activity in murine B16F0 melanoma cells. The structural relationship of active compounds was discussed.

We investigated the anti-inflammatory effects of 3α-hydroxy-lup-20(29)-en-23, 28-dioic acid (HLEDA)—a lupane-type triterpene isolated from leaves of Acanthopanax gracilistylus W. W.Smith (AGS), as well as the underlying molecular mechanisms in lipopolysaccharide (LPS)-induced RAW264.7 cells. Our results demonstrated that HLEDA concentration-dependently reduced the production of nitric oxide (NO), significantly suppressed LPS-induced expression of TNF-α and IL-1β at the mRNA and protein levels in RAW264.7 cells. Further analysis revealed that HLEDA could reduce the secretion of High Mobility Group Box 1 (HMGB1). Additionally, the results showed that HLEDA efficiently decreased nuclear factor-kappaB (NF-κB) activation by inhibiting the degradation and phosphorylation of IκBα. These results suggest that HLEDA exerts anti-inflammatory properties in LPS-induced macrophages, possibly through inhibition of the NF-κB signaling pathway, which mediates the expression of pro-inflammatory cytokines. These results warrant further studies that would concern candidate therapy for diseases, such as fulminant hepatitis and rheumatology of triterpenoids in AGS.

Background: White ginseng (Panax ginseng Meyer) is commonly distributed as a health food in food markets. However, there is no practical method for distinguishing Korean white ginseng (KWG) from Chinese white ginseng (CWG), except for relying on the traceability system in the market. Methods: Ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry combined with orthogonal partial least squares discrimination analysis (OPLS-DA) was employed to discriminate between KWG and CWG. Results: The origins of white ginsengs in two test sets (1.0 μL and 0.2 μL injections) could be successfully discriminated by the OPLS-DA analysis. From OPLS-DA S-plots, KWG exhibited tentative markers derived from ginsenoside Rf and notoginsenoside R3 isomer, whereas CWG exhibited tentative markers derived from ginsenoside Ro and chikusetsusaponin Iva. Conclusion: Results suggest that ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry coupled with OPLS-DA is an efficient tool for identifying the difference between the geographical origins of white ginsengs.

A new megastigmane glycoside, galloyl linarionoside A (1), together with 13 known compounds (2-14) were isolated from the aerial parts of Aceriphyllum rossii ENGLER. (Saxifragaceae). The chemical structures of the isolated compounds were established mainly by using nuclear magnetic resonance spectra, mass spectrometry, and modified Mosher's method. Among the isolates, compounds 4, 5, 6 and 7 showed potent inhibitory activity against the lipopolysaccharide-induced nitric oxide production in RAW264.7 macrophage cells with IC50 values of 12.5, 9.5, 10.5 and 9.3 µM, respectively. The anti-inflammatory effect of compound 7 was accompanied by dose-dependent decreases in the production of inducible nitric oxide synthase and cyclooxygenase-2 proteins not in the inhibitor kappa B (IκB)-dependent nuclear factor-kappa B activation.

Mitogen-activated protein kinases play a key role in cell proliferation, cell cycle progression and cell transformation, and activated Ras/extracellular signal-regulated kinases (ERKs)/ribosomal S6 kinase 2 (RSK2) signaling pathways have been widely identified in many solid tumors. In this study, we found that magnolin, a compound found in the Magnolia species, directly targeted and inhibited ERK1 and ERK2 kinase activities with IC50 values of 87 and 16.5 nM by competing with adenosine triphosphate in an active pocket. Further, we demonstrated that magnolin inhibited epidermal growth factor (EGF)-induced p90RSKs phosphorylation at Thr359/Ser363, but not ERKs phosphorylation at Thr202/Tyr204, and this resulted in inhibition of cell proliferation by suppression of the G1/S cell cycle transition. Additionally, p38 kinases, Jun N-terminal kinases and Akts were not involved in the magnolin-mediated inhibitory signaling. Magnolin targeting of ERK1 and 2 activities suppressed the phosphorylation of RSK2 and downstream target proteins including ATF1 and c-Jun and AP-1, a dimer of Jun/Fos, and the transactivation activities of ATF1 and AP-1. Notably, ERKs inhibition by magnolin suppressed EGF-induced anchorage-independent cell transformation and colony growth of Ras(G12V)-harboring A549 human lung cancer cells and NIH3T3 cells stably expressing Ras(G12V) in soft agar. Taken together, these results demonstrated that magnolin might be a naturally occurring chemoprevention and therapeutic agent capable of inhibiting cell proliferation and transformation by targeting ERK1 and ERK2.

Two new triterpenes, (1α,3β,8α,9β,10α,13α,14β)-9,10-dimethyl-25,26-dinorolean-5-en-1,3-diol (1) and (1α,3β,6β)-olean-12-en-1,3,6-triol (2) were isolated from the leaves of Aleurites fordii, together with five known triterpenes. The structures of isolates were established by one dimensional (1D)- and 2D-NMR spectroscopic data along with MS analysis. Of the isolated compounds, 1, 2 and 4 (daturadiol) displayed moderate cytotoxicities against two or more human cancer cell lines in HepG2 (hepatocellular carcinoma), SK-OV-3 (ovarian carcinoma), A-549 (lung carcinoma) and SNU-1 (gastric carcinoma).

Bioactivity-guided fractionation for an EtOAc-soluble fraction of methanolic extract of Arthraxon hispidus, using primary cell assay with bone marrow-derived mast cells (BMMC), led to an isolation of six new flavones and nine known compounds. The structures of the new compounds were established by one dimensional (1D)- and 2D-NMR spectroscopic data, as luteolin 8-C-β-kerriopyranoside (1), luteolin 8-acetic acid methyl ester (2), 7-methyl-luteolin 8-C-β-(6-deoxyxylo-3-uloside) (3), apigenin 8-C-α-fucopyranoside (4), apigenin 8-C-β-fucopyranoside (5) and luteolin 8-C-β-fucopyranoside (6). All the isolates were evaluated for inhibitory activities on interleukin-6 release in the primary cultures using BMMC. Of the tested compounds, compounds 2, 3 and 10 were found to inhibit interleukin-6 release. Furthermore, compound 2 displayed inhibitory activity against prostaglandin D2, leukotriene C4, and β-hexosaminidase releases.

Melanin plays an important role in protecting the skin against ultraviolet light and is responsible for skin color. However, overproduction of melanin is related to several skin disorders, such as age spots, freckles, cafe au lait spots, Becker’s nevus and other hyperpigmentation syndromes. The aim of this study was to identify the effects of kaempferol-7-O-β-d-glucuronide (K7G) and tilianin, isolated from Cryptotaenia japonica, on melanogenesis and their mechanisms of action in murine B16 melanoma cells. The α-melanocyte-stimulating hormone (α-MSH)-induced melanin production was significantly inhibited by K7G and tilianin in a dose-dependent manner. The effects of these compounds on the signaling pathway of melanogenesis were examined. K7G and tilianin downregulated the expression of microphthalmia-associated transcription factor (MITF) and melanocyte-specific enzymes, i.e., tyrosinase and TRP1. These compounds also inhibited the phosphorylation of cyclic adenosine monophosphate (cAMP)-response element binding protein (CREB) in a dose-dependent manner. In addition, these compounds increased the phosphorylation of extracellular signal-regulated kinase (ERK) but decreased the phosphorylation of c-Jun N-terminal kinase (JNK) in B16 cells. Based on the above results, the anti-melanogenic effects of these compounds are caused by suppression of the MAPK signaling pathway through the down-regulation of α-MSH-induced CREB accumulation. This finding suggests that K7G and tilianin may be good candidates for further research to develop therapeutic agents for hyperpigmentation diseases.

IEEE 802.11 Wireless Local Area Network (WLAN) supports multiple transmission rates according to the channel condition. In multi-rate IEEE 802.11 WLAN, the performance of stations with high rates may decline due to the relatively long channel occupation time of the stations with low rates. In order to mitigate this performance anomaly problem, we propose a new Medium Access Control (MAC) protocol. In the protocol, after the Access Point (AP) identifies the IDs of the near stations around the AP, it allocates time slots to the stations in the vicinity of the AP. Then they transmit data packets at the allocated time slots in a non-contention manner using the physical scheme of Wi-Fi. Through the simulation results, we show that the throughput of the proposed MAC protocol is superior to that of the traditional IEEE 802.11g by guaranteeing transmission opportunities of the stations near the AP.

Objectives The effects of β-catenin promoter haplotypes on its mRNA expression levels and asthma risks were investigated in Korean subjects. Design and methods The genotype analyses were conducted by a Taqman method for 684 Korean subjects, 400 controls and 284 with asthma. Measurement of mRNA expression levels in peripheral blood nucleated cells were conducted on subjects whose buffy coat fractions were available (n = 185). Logistic regression analyses were conducted to test the associations of the β-catenin promoter haplotypes with asthma risks. Results Four SNPs, − 10,288C>T (rs7630377), − 6,426C>G (rs9859392), − 4,361G>C (rs9870255), and − 765G>A (rs3864004), were identified in the promoter region of the β-catenin gene, and three common haplotypes were constructed from them. Haplotype ht1[CCGG] was associated with decreased β-catenin mRNA expression levels and a lower asthma risk with an odds ratio of 0.53, while ht2[TGCA] was associated with increased mRNA expression levels and a higher asthma risk with an odds ratio of 2.34. Ht3[TCGG] had no significant effects on both. Conclusions Our findings show that β-catenin promoter polymorphism affects its mRNA expression levels, and also is significantly associated with the asthma risk of Korean subjects.

Mangosteen ( Garcinia mangostana L.), one of top-selling botanical dietary supplements in the USA, has been used as food and folk medicines in southeastern Asia. Herein, α-and γ-mangostins, major constituents of mangosteen, were investigated for their effect on the bone marrow-derived mast cell (BMMC) mediated allergy mechanism induced by phorbol 12-myristate 13-acetate (PMA) plus A23187 . α- and γ-mangostins demonstrated to inhibit Interleukin (IL)-6, prostaglandin D 2 (PGD 2 ) and leukotriene C 4 (LTC 4 ) production as well as degranulation in PMA plus A23187 induced BMMC. Furthermore, α- and γ-mangostins were found to repress cyclooxygenase (COX)-2 expression in the present study. Thus, these results suggest that α- and γ-mangostins may be useful in alleviating mast cell-mediated allergic inflammatory responses.

A new ingenane-type diterpene, (3S,5R)5-O-(2,3-dimethylbutanoyl)-13-O-dodecanoyl-20-O-deoxyingenol (1), and six known compounds,3-O-(2,3-dimethylbutanoyl)-13-O-dodecanoyl-20-O-deoxyingenol (2), 20-O-decanoylingenol (3), 20-O-acetylingenol-3-O-(2'E,4'Z) decadienoate (4), kansuiphorin A (5), 3-O-(2,3-dimethylbutanoyl)-13-O-dodecanoylingenol (6), and kansuinin F (7) were isolated and evaluated for their effect on IFN-γ production in NK92 cells. Interestingly, subjection to compounds 4 and 6 (10 nM) displayed the most significant response in IFN-γ production, comparable to that produced by the same dose of phorbol 12-myistate 13-acetate (PMA). High doses of compounds 3 (100 nM), 1 (1. 25 μM) and 5 (5.0 μM) have also been shown to activate the IFN-γ production.

Skullcapflavone II is a flavonoid derived from Scutellaria baicalensis, a widely used herbal medicine in anti-inflammatory and anticancer therapy in Korea. Skullcapflavone II antagonized the bradykinin receptor more potently than any of the other flavonoids derived from this plant. Here, we were investigated its therapeutic effects in a mouse model of ovalbumin (OVA)-induced allergic asthma. Administration of skullcapflavone II significantly reduced airway hyperresponsiveness (AHR), airway eosinophilia, Th2 cytokine production, and increased transforming growth factor-β1 (TGF-β1) levels in bronchoalveolarlavage (BAL) fluids and lungs from OVA-sensitized and -challenged mice. Skullcapflavone II administration also significantly suppressed subepithelial collagen deposition and goblet cell hyperplasia, elevated Smad7 expression and suppressed pSmad2/3 levels. Collectively, these findings indicate that skullcapflavone II, a potential bradykinin antagonist, reduced the major pathophysiological features of allergic asthma, at least in part by acting on TGF-β1/Smad signaling pathways. Thus, skullcapflavone II may have therapeutic potential for the treatment of allergic asthma.