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더덕(Codonopsis lanceolata)은 주로 한국, 중국 등 동아시아 지역에 재배되고 있으며, 더덕의 뿌리는 기침, 기관지염, 천식, 결핵, 소화 불량의 증상을 치료하기 위한 기능성 식품 및 전통 의학으로 사용되어져 왔다. 보고된 바에 의하면 phenylpropanoids, polyacetylenes, saponins, flavonoids와 같은 다양한 식물 천연물 성분들이 항비만, 항염, 항암, 항산화, 항미생물 활성과 같은 약리학적 작용에 관여한다고 보고되어 있다. MS기반 대사체학 분석을 이용한 주산지의 마커 성분을 선정하는 것은 다른 지역에서 재배된 약용 식물의 안전성뿐만 아니라 화학적 조성과 생물학적 효능의 변화와도 관련이 있기 때문에 부작용 없이 더덕의 유익한 효과만을 보장하는데 중요하다. 본 연구에서는 국내산 더덕의 주산지 특성을 구별하기 위해 UPLC-QTOF-MS를 기반으로 하는 대사체 프로파일링과 다변량 통계분석 기법인 PCA 분석을 수행하여 판별모델을 확립하였다. 그 결과 인제(강원도), 횡성(강원도), 무주(전라북도)의 3개 그룹이 PCA와 loading plot 분석결과 tangshenoside I, lancemaside A, lancemaside G는 더덕 주산지를 구별하기 위한 잠재적 대사체 마커들로 제안하였다.

본 연구는 황기와 지치 복합물인 ALM16이 lipopolysaccharide 처리에 의해 자극된 RAW264.7 대식세포의 염증반응에 미치는 영향에 대하여 조사하였다. ALM16은 RAW264.7 대식세포에 대하여 최대 200 μg/mL의 농도까지 독성은 보이지 않았다. 항염증 활성을 검정하기 위해 nitric oxide (NO), prostaglandin E2 (PGE2) 및 pro-inflammatory cytokines 생성량을 측정한 결과, ALM16은 각각의 생성량을 농도의존적으로 감소시켰다. 또한 ALM16은 NO와 PGE2 생성에 관여하는 inducible nitric oxide synthase (iNOS)와 cyclooxygenase-2 (COX-2)의 단백질 발현을 억제하였다. 한편, 항염증 활성 조절 기전을 확인하기 위하여 NK-kB의 핵으로의 이동과 DNA-binding activity 및 MAPK 신호전달 경로에 대한 ALM16의 영향을 확인한 결과, ALM16은 NF-κB의 핵으로 이동과 DNA-binding activity를 유의적으로 억제하였으며, JNK와 ERK 특이적으로 인산화를 억제함으로써 MAPK 신호전달 경로 활성을 억제하였다. 이러한 결과를 종합하여 볼 때 ALM16이 MAPK와 NF-κB의 신호전달 경로 억제를 통한 iNOS와 COX-2의 발현을 조절하고, 이로 인하여 NO, PGE2 및 pro-inflammatory cytokines의 생성이 감소하여 염증 반응을 조절하는 능력이 있는 것으로 판단된다.

Whistler-mode chorus and electromagnetic ion cyclotron waves have long been considered major causes of electron flux changes in the Earth’s outer radiation belt. Here, we report an ideal observation event from two identical satellites, during which the electron flux significantly decreases, followed by a partial recovery under the simultaneous existence of both waves at the same location. The electron flux changes are mostly consistent with predictions from scattering by both waves. We suggest that the combined scattering effect of these two types of waves can be addressed more accurately by a full test particle simulation rather than the current prevailing quasilinear resonant diffusion approach.

Brugmansia arborea L. (Solanaceae), commonly known as "angel's trumpet," is widely grown in North America, Africa, Australia, and Asia. It has been mainly used for ornamental purposes as well as analgesic, anti-rheumatic, vulnerary, decongestant, and anti-spasmodic materials. B. arborea is also reported to show anti-cholinergic activity, for which many alkaloids were reported to be principally responsible. However, to the best of our knowledge, a phytochemical study of B. arborea flowers has not yet been performed. Four flavonol glycosides (1-4) and one dihydroflavanol (5) were for the first time isolated from B. arborea flowers in this study. The flavonoids showed significant antioxidant capacities, suppressed nitric oxide production in lipopolysaccharide (LPS)-treated RAW 264.7 cells, and reduced inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX-2) protein production increased by LPS treatment. The contents of compounds 1-4 in n-BuOH fraction were determined to be 3.8 ± 0.9%, 2.2 ± 0.5%, 20.3 ± 1.1%, and 2.3 ± 0.4%, respectively, and that of compound 5 in EtOAc fraction was determined to be 12.7 ± 0.7%, by HPLC experiment. These results suggest that flavonol glycosides (1-4) and dihydroflavanol (5) can serve as index components of B. arborea flowers in standardizing anti-inflammatory materials.

Microbial cellulases have become the mainstream biocatalysts due to their complex nature and widespread industrial applications. Here, homogeneous endoglucanase GluCB31 from Bacillus subtilis subsp. inaquosorum CBS31 was studied. GluCB31 was purified to 17.68-fold with an 8.33% yield and a specific activity of 1066.37 U/mg. Biochemical properties of GluCB31 were performed and the results are as follows; molecular mass of 35 kDa with an optimum pH at 7.5 and temperature at 50°C. GluCB31 was immobilized in calcium alginate gel and it exhibited the highest activity at 10°C higher temperature than soluble enzyme, as the entrapment in alginate gel made GluCB31 more stable. Kinetic studies showed the Vmax of 1293.33 ± 2.51 U/mg and Km of 0.0183 mg/mL. Enzymatic activity was activated by Tween-20 (106.7%), Tween-80 (111.6%), Triton X-100 (142.3%), SDS (135.5%), Mg++ (185.7%), Cu++ (167.6%), Zn++ (153.7%), Mn++ (106.3%), Ba++ (181.9%), Ni++ (107.2%) while inhibited by Fe++ (15.8%), β-mercaptoethanol (46.8%), EDTA (54.5%). Enthalpy, free energy, and entropy of activation were calculated to be 38.526 kJmol-1, 44.187 kJmol-1, and -17.518 Jmol-1K-1 respectively. Also, ΔGE-S and ΔGE-T were found to be -10.75 kJmol-1 and -45.92 kJmol-1 respectively. A low ΔS, ΔGE-S, and ΔGE-T values were signified enzyme-catalyzed reaction occurs at a fast rate and the existence of the enzyme in its stable state. Cellobiose was the major end product of hydrolysis. These attributes of GluCB31 demonstrated the diversity of catalytic activities and serve in various biotechnological processes, thus deserve to be developed as a bio-industrial agent.

The extract from Cnidium officinale rhizomes was shown in a prior experiment to markedly recover otic hair cells in zebrafish damaged by neomycin. The current study was brought about to identify the principal metabolite. Column chromatography using octadecyl SiO2 and SiO2 was performed to isolate the major metabolites from the active fraction. The chemical structures were resolved on the basis of spectroscopic data, including NMR, IR, MS, and circular dichroism (CD) data. The isolated phthalide glycosides were assessed for their recovery effect on damaged otic hair cells in neomycin-treated zebrafish. Three new phthalide glycosides were isolated, and their chemical structures, including stereochemical characteristics, were determined. Two glycosides (0.1 μM) showed a recovery effect (p < 0.01) on otic hair cells in zebrafish affected by neomycin ototoxicity. Repeated column chromatography led to the isolation of three new phthalide glycosides, named ligusticosides C (1), D (2), and E (3). Ligusticoside C and ligusticoside E recovered damaged otic hair cells in zebrafish.

Cnidium officinalis rhizomes were immersed in 80% MeOH. The extract was fractionated to water, n-butanol, and ethyl acetate fractions (Fr). Open column chromatography was repeatedly carried out on n-butanol and ethyl acetate Fr using silica gel, octadecyl silica gel, and Sephadex LH-20 as the stationary phase affording five phenyl alkanoids 1–5 including two new ones. The molecular structures including stereochemistry were decided based on spectroscopic interpretation of nuclear magnetic resonance, mass spectrometry, and infrared spectroscopy as well as chemical reaction. Three known compounds, coniferyl alcohol methyl ether (1), vanillin (2), and coniferyl aldehyde (3), were reported in the beginning for this plant by authors. Two new phenyl alkanoids were named, 7-methoxyeugenol and cnidiumoside.

Acanthopanax sessiliflorus (Araliaceae) have been reported to exhibit many pharmacological activities. Our preliminary study suggested that A. sessiliflorus fruits include many bioactive 3,4-seco-triterpenoids. A. sessiliflorus fruits were extracted in aqueous EtOH and fractionated into EtOAc, n-BuOH, and H2O fractions. Repeated column chromatographies for the organic fractions led to the isolation of 3,4-seco-triterpenoid glycosides, including new compounds. Ultra-high-performance liquid chromatography (UPLC) mass spectrometry (MS) systems were used for quantitation and quantification. BV2 and RAW264.7 cells were induced by LPS, and the levels of pro-inflammatory cytokines and mediators and their underlying mechanisms were measured by ELISA and Western blotting. NMR, IR, and HR-MS analyses revealed the chemical structures of the nine noble 3,4-seco-triterpenoid glycosides, acanthosessilioside G–O, and two known ones. The amounts of the compounds were 0.01–2.806 mg/g, respectively. Acanthosessilioside K, L, and M were the most effective in inhibiting NO, PGE2, TNF-α, IL-1β, and IL-6 production and reducing iNOS and COX-2 expression. In addition, it had inhibitory effects on the LPS-induced p38 and ERK MAPK phosphorylation in both BV2 and RAW264.7 cells. Nine noble 3,4-seco-triterpenoid glycosides were isolated from A. sessiliflorus fruits, and acanthosessilioside K, L, and M showed high anti-inflammatory and anti-neuroinflammatory effects.

A new neolignan glucoside has been isolated from Chrysanthemum morifolium ‘Baekma’ cultivar through repeated silica gel and octadecyl silica gel (ODS) column chromatographies. On the basis of spectroscopic data including NMR, MS, and IR, the chemical structure of the new neolignan glucoside was determined to be (7S,8S)-7-O-[1′-(4′,5′-dihydroxy-3′-methoxyphenyl)propanol]guaiacylglycerol 4-O-β-D-glucopyranoside (1), named baekmaoside A.

꼬리겨우살이(Loranthus tanakae) 전초를 80% MeOH 수용액으로 4회 반복 추출한 뒤, 감압 농축한 추출물을 ethyl acetate(EtOAc), n-butyl alcohol (n-BuOH)과 H2O층으로 계통 분획을 실시하였다. n-BuOH 분획에 대하여 silica gel (SiO2), octadecyl silica gel (ODS), Sephadex LH-20 column chromatographies를 반복실시하여 1종의 cyclofarnesane sesquiterpene glucoside 화합물을 분리 및 정제하였다. 스펙트럼 데이터를 분석하여 입체 구조를 포함한 화합물의 구조를 (1''R,3''S,5''R, 8''S,2E,4E)-dihydrophaseic acid 3''-O-β-D-glucopyranoside로 구조동정 하였다. 이 화합물은 이번 실험을 통하여 꼬리겨우살이로부터는 최초로 분리되었다. 분리한 단일 물질은 AGS (Caucasian gastric adenocarcinoma cells)와 Hepatocyte carcinoma cells에 대하여 50 μg/mL 이상에서 농도 의존적으로 유의한 정도의 세포독성을 보이는 것이 확인되었다.

Begonia semperflorens Link et Otto has been broadly raised up for ornamental purpose as well comestible blossom. As the reproductive structures of phanerogams, flowers contain various secondary metabolites and have many biological activities. Accordingly, we began the contrivance for isolation and analysis of flavonoids contained in B. semperflorens flowers. MeOH extraction of B. semperflorens followed solvent fractionation was prosecuted. Column chromatography of non-polar fraction gave four flavonoids using several resins. Identification of the flavonols were established as quercetin (1), kaempferol (2), astragalin (3), and isoquercetin (4) by interpreting a variety of spectral information. Quercetin (1) and kaempferol (2) inhibited NO production and protected against t-BHP-induced oxidative stress. Kaempferol (2) also protected cell death of glutamate-treated HT22. Quantitative analysis of flavonoid content in B. semperflorens flowers was also performed using HPLC experiment.

Repeated column chromatography using Sephadex LH-20, silica gel (SiO2), and octadecyl SiO2 (ODS) as well as preparative HPLC column chromatography led to isolation of a new dibenzocyclooctadiene lignan along with four known ones, gomisin L2 (1), L1 (2), M1 (3), and M2 (4). Their chemical structures were fixed based on MS, IR, and NMR data analyses. In addition, the stereochemistry of atropisomers, the absolute configuration of the axial chirality in a biphenyl structure, was confirmed by a CD experiment. The new lignan was named gomisin M3 (5).

An amendment to this paper has been published and can be accessed via the original article.

Non-alcoholic fatty liver disease (NAFLD) is a disease associated with metabolic syndromes such as diabetes and obesity, regardless of alcohol consumption, and refers to the accumulation of triacylglycerols in the liver. Thymol (THY) is a vegetable essential oil that is naturally contained in the Zingiberaceae and Lamiaceae families. THY was isolated from Curcuma longa L. The rhizomes of Curcuma longa L. were dried, sliced and extracted with 50% ethanol and then isolated through repeated column chromatography. This study was conducted to investigate the inhibitory effect of THY, even in non-alcoholic fatty liver disease, in relation to the inhibiting hyperlipidemia effect of THY, which was demonstrated in previous studies. Hepatocytes were treated with oleate (OA) containing THY to observe lipid accumulation by Oil Red O staining (ORO). We also tested the effect of THY on triacylglycerols (TG) and total cholesterol (TC) in HepG2 cells. Western blot and real-time RT-PCR using sterol regulatory element-binding protein-1c (SREBP-1c), fatty acid synthase (FAS), acetyl-CoA carboxylase (ACC), CCAAT-enhancer-binding protein (C/EBP), proliferator-activated receptor &gamma, (PPAR&gamma, ), and adenosine monophosphate (AMP)-activated protein kinase (AMPK) expressions were carried out. Consequently, inhibition of lipogenesis by THY (100 &mu, M or 200 &mu, M) in NAFLD treated with OA in HepG2 cells was confirmed. The results of TG and TC experiments confirmed a decrease in the degree of fat accumulation in the liver. Furthermore, inhibition of the SREBP-1c, FAS, ACC, C/EBP and PPAR&gamma, expressions that mediated fat accumulation and increased AMPK phosphorylation was observed. Taken together, THY is proposed as a potential natural constituent for the treatment of NAFLD.

Repeated chromatographic separations of the EtOAc fraction of Schisandra chinensis fruits on silica gel, octadecyl silica gel, and Sephadex LH-20 led to the isolation and identification of seven dibenzocyclooctadiene lignans (1–7). The NMR data reported in the literature for angeloyl gomisin H (5) were shown to be incorrect. We unambiguously identified the compounds based on detailed analysis of the 1D and 2D NMR data, especially from HMBC and NOESY experiments. In addition, MTT assays and cell viability experiments verified the cytotoxicity of the isolated dibenzocyclooctadiene lignans against the human cancer cell lines AGS, HeLa, and HT-29.

Triterpenoid saponins (TSs) are common plant defense phytochemicals with potential pharmaceutical properties. Platycodon grandiflorus (Campanulaceae) has been traditionally used to treat bronchitis and asthma in East Asia. The oleanane-type TSs, platycosides, are a major component of the P. grandiflorus root extract. Recent studies show that platycosides exhibit anti-inflammatory, antiobesity, anticancer, antiviral, and antiallergy properties. However, the evolutionary history of platycoside biosynthesis genes remains unknown. In this study, we sequenced the genome of P. grandiflorus and investigated the genes involved in platycoside biosynthesis. The draft genome of P. grandiflorus is 680.1 Mb long and contains 40,017 protein-coding genes. Genomic analysis revealed that the CYP716 family genes play a major role in platycoside oxidation. The CYP716 gene family of P. grandiflorus was much larger than that of other Asterid species. Orthologous gene annotation also revealed the expansion of β-amyrin synthases (bASs) in P. grandiflorus, which was confirmed by tissue-specific gene expression. In these expanded gene families, we identified key genes showing preferential expression in roots and association with platycoside biosynthesis. In addition, whole-genome bisulfite sequencing showed that CYP716 and bAS genes are hypomethylated in P. grandiflorus, suggesting that epigenetic modification of these two gene families affects platycoside biosynthesis. Thus whole-genome, transcriptome, and methylome data of P. grandiflorus provide novel insights into the regulation of platycoside biosynthesis by CYP716 and bAS gene families.

(1) Background: Many flavonoids derived from natural sources have been reported to exhibit antioxidant and anti-inflammatory effects. Our preliminary study suggested that Coreopsis lanceolata flowers (CLFs) include high flavonoid content, (2) Methods: CLFs were extracted in 80% (v/v) aqueous methanol and fractionated into ethyl acetate, n-butanol, and water fractions. Repeated column chromatographies for the organic fractions led to the isolation of seven flavanones. Quantitative analysis of the flavanones was carried out using reversed-phase high-performance liquid chromatography. All flavanones were evaluated for their antioxidant and pro-inflammatory inhibition effects, (3) Results: Spectroscopic analyses revealed the chemical structure of five new flavanones, coreolanceolins A&minus, E, and two known ones. The content of the seven flavanones in extracts were determined from 0.8 &plusmn, 0.1 to 38.8 &plusmn, 0.3 mg/g. All flavanones showed radical scavenging activities (respectively 104.3 &plusmn, 1.9 to 20.5 &plusmn, 0.3 mg vitamin C equivalents (VCE)/100 mg and 1278.6 &plusmn, 26.8 to 325.6 &plusmn, 0.2 mg VCE/100 mg) in the DPPH and 2,2&prime, Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays and recovery activities in Caco-2 (59.7 to 41.1%), RAW264.7 (87.8 to 56.0%), and PC-12 (100.5 to 69.9%) cells against reactive oxygen species. Furthermore, all flavanones suppressed nitric oxide production (99.5% to 37.3%) and reduced iNOS and COX-2 expression in lipopolysaccharide-treated RAW 264.7 cells, (4) Conclusions: Five new and two known flavanones were isolated from CLF, and most of them showed high antioxidant and pro-inflammatory inhibition effects.

Efforts to isolate a broad-spectrum antimicrobial peptide (AMP) from microbial sources have been on the rise recently. Here, we report the identification, the optimization of the culture conditions, and the characterization of an efficient AMP from the Bacillus strain designated MS07 that exhibits antimicrobial and antibiofilm activity. The production of MS07 was maximized by evaluating the culture conditions by the response surface methodology to obtain optimum media compositions. The biochemical integrity of MS07 was assessed by a bioassay indicating inhibition at ~6 kDa, like tricine-SDS-PAGE. MALDI-TOF confirmed the molecular weight and purity, showing a molecular mass of 6.099 kDa. Peptide MS07 exhibited antimicrobial activity against both Gram-positive and Gram-negative bacteria. The MIC of MS07 for Escherichia coli, Alcaligenes faecalis, MRSA, and Pseudomonas aeruginosa ranged from 16&ndash, 32 &micro, g/mL, demonstrating superior potency. The biomass was diminished by about 15% and 11%, with rising concentrations up to 8 &times, MIC, for P. aeruginosa and E. coli biofilm, respectively. MS07 exhibited an 8 &micro, M and 6 &micro, M minimum bactericidal concentration against the biofilm of the Gram-negative strains P. aeruginosa and E. coli, respectively. Peptide MS07 reduced and interrupted the biofilm development in a concentration-dependent manner, as determined by BacLight live/dead staining using confocal microscopy.

A repeated column chromatography for Forsythia koreana Nakai. flowers afforded a phenylethane glycoside, which was identified as 8′-(3,4-dihydroxyphenyl)ethyl-O-α-l-rhamnopyranosyl-(1 → 4)-2-O-(E)-caffeoyl-α-l-arabinopyranoside based on spectroscopic analyses of 1D NMR (1H-NMR, 13C-NMR, DEPT), 2D NMR (gCOSY, gHSQC, gHMBC), FAB/MS, specific rotation, and IR spectrometry. This compound was isolated from F. koreana flower for the first time in this study. The compound showed scavenge activities in ORAC and DPPH radicals with the values of 0.83 ± 0.01 and 84.66 ± 0.75% (at the concentration of 500 ppm), respectively. It also inhibited production of NO for RAW 264.7 stimulated by LPS and protected oxidative stress induced by glutamate in HT22-immortalized hippocampal. The IC50 on inhibition of NO production and EC50 value on protective efficacy of oxidative stress were 78.72 ± 1.43 μM and 176.25 ± 7.23 μM, respectively. These results demonstrate that the phenylethanoid glycoside might be useful as a neuroprotective agent because of their antioxidant, anti-inflammatory, and neuroprotective effects.

Aglycon protopanaxatriol (APPT) has valuable pharmacological effects such as memory enhancement and tumor inhibition. β-Glycosidase from the hyperthermophilic bacterium Dictyoglomus turgidum (DT-bgl) hydrolyzes the glucose residues linked to APPT, but not other glycoside residues. β-Glycosidase from the hyperthermophilic bacterium Pyrococcus furiosus (PF-bgl) hydrolyzes the outer sugar at C-6 but not the inner glucose at C-6 or the glucose at C-20. Thus, the combined use of DT-bgl and PF-bgl is expected to increase the biotransformation of PPT-type ginsenosides to APPT. We optimized the ratio of PF-bgl to DT-bgl, the concentrations of substrate and enzyme, and the reaction time to increase the biotransformation of ginsenoside Re and PPT-type ginsenosides in Panax ginseng leaf extract to APPT. DT-bgl combined with PF-bgl converted 1.0 mg/ml PPT-type ginsenosides in ginseng leaf extract to 0.58 mg/ml APPT without other ginsenosides, with a molar conversion of 100%. We achieved the complete biotransformation of ginsenoside Re and PPT-type ginsenosides in ginseng leaf extract to APPT by the combined use of two β-glycosidases, suggesting that discarded ginseng leaves can be used as a source of the valuable ginsenoside APPT. To the best of our knowledge, this is the first quantitative production of APPT using ginsenoside Re, and we report the highest concentration and productivity of APPT from ginseng extract to date.

A new lignan (1) was isolated from the flowers of Forsythia koreana along with one known lignan, 4,4′-di-O-β-D-glucosylpinoresinol (2). The molecular structures were determined using spectral methods. These compounds were isolated from F. koreana flowers for the first time.

A simple method to prepare a high-content rutin fraction from Forsythia koreana flowers (HRFK) is described. Rutin, isolated for the first time from the flowers, was identified from spectroscopic data including nuclear magnetic resonance, mass spectrometry, and infrared. As a result of HPLC quantitative analysis, the content of rutin was found to be 80.0 ± 0.02% in HRFK. Our previous study reported that F koreana MeOH extract (FK) significantly recovered alloxan-induced pancreatic islets in zebrafish. However, HRFK as well as rutin exhibited an enhanced anti-diabetic effect compared to FK in our latest experiments. In conclusion, HRFK, as well as rutin and FK, have potential as anti-diabetic agents.

Three phenylpropanoids were isolated from the flowers of Lilium Asiatic hybrids through repeated silica gel or octadecyl silica gel column chromatographies. The chemical structures were determined to be 1-O-trans-caffeoyl-β-d-glucopyranoside (1), regaloside A (2), and regaloside B (3), based on spectroscopic data gathered from nuclear magnetic resonance (NMR) spectroscopy, electron ionization mass spectrometry (EI/MS), polarimetry, and infrared spectroscopy (IR) experiments. Compounds 1 and 2 showed significant DPPH radical scavenging activity of 60.1 and 58.0% at 160 ppm, respectively, compared with the 62.0% activity of the positive control, α-tocopherol. At a concentration of 50 μg/mL, compounds 1–3 inhibited the expression of iNOS to 4.1 ± 0.01, 70.3 ± 4.07, and 26.2 ± 0.63, respectively, and decreasing COX-2 expression to 67.8 ± 4.86, 131.6 ± 8.19, and 98.9 ± 4.99. Also, at the same concentration, compounds 1–3 decreased the ratio of p-p65/p-65 to 43.8 ± 1.67, 40.7 ± 1.30, and 43.2 ± 1.60, respectively, and the expression of VCAM-1 to 42.1 ± 2.31, 48.6 ± 2.65, and 33.8 ± 1.74, respectively.

Nature demonstrates adaptive and extreme shape morphing via unique patterns of movement. Many of them have been explained by monolithic shape-changing mechanisms, such as chemical swelling, skin stretching, origami/kirigami morphing, or geometric eversion, that were successfully mimicked in artificial analogs. However, there still remains an unexplored regime of natural morphing that cannot be reproduced in artificial systems by a "single-mode" morphing mechanism. One example is the "dual-mode" morphing of Eurypharynx pelecanoides (commonly known as the pelican eel), which first unfolds and then inflates its mouth to maximize the probability of engulfing the prey. Here, we introduce pelican eel-inspired dual-morphing architectures that embody quasi-sequential behaviors of origami unfolding and skin stretching in response to fluid pressure. In the proposed system, fluid paths were enclosed and guided by a set of entirely stretchable origami units that imitate the morphing principle of the pelican eel's stretchable and foldable frames. This geometric and elastomeric design of fluid networks, in which fluid pressure acts in the direction that the whole body deploys first, resulted in a quasi-sequential dual-morphing response. To verify the effectiveness of our design rule, we built an artificial creature mimicking a pelican eel and reproduced biomimetic dual-morphing behavior. By compositing the basic dual-morphing unit cells into conventional origami frames, we demonstrated architectures of soft machines that exhibit deployment-combined adaptive gripping, crawling, and large range of underwater motion. This design principle may provide guidance for designing bioinspired, adaptive, and extreme shape-morphing systems.

BackgroundOsteoarthritis (OA) is an age-related joint disease with characteristics that involve the progressive degradation of articular cartilage and resulting chronic pain. Previously, we reported thatAstragalus membranaceusandLithospermum erythrorhizonshowed significant anti-inflammatory and anti-osteoarthritis activities. The objective of this study was to examine the protective effects of ALM16, a new herbal mixture (7:3) of ethanol extracts ofA. membranaceusandL. erythrorhizon,against OA in in vitro and in vivo models.MethodsThe levels of matrix metalloproteinase (MMP)-1, −3 and − 13 and glycosaminoglycan (GAG) in interleukin (IL)-1β or ALM16 treated SW1353 cells were determined using an enzyme-linked immunosorbent and quantitative kit, respectively. In vivo, the anti-analgesic and anti-inflammatory activities of ALM16 were assessed via the acetic acid-induced writhing response and in a carrageenan-induced paw edema model in ICR mice, respectively. In addition, the chondroprotective effects of ALM16 were analyzed using a single-intra-articular injection of monosodium iodoacetate (MIA) in the right knee joint of Wister/ST rat. All samples were orally administered daily for 2 weeks starting 1 week after the MIA injection. The paw withdrawal threshold (PWT) in MIA-injected rats was measured by the von Frey test using the up-down method. Histopathological changes of the cartilage in OA rats were analyzed by hematoxylin and eosin (H&E) staining.ResultsALM16 remarkably reduced the GAG degradation and MMP levels in IL-1β treated SW1353 cells. ALM16 markedly decreased the thickness of the paw edema and writhing response in a dose-dependent manner in mice. In the MIA-induced OA rat model, ALM16 significantly reduced the PWT compared to the control group. In particular, from histological observations, ALM16 showed clear improvement of OA lesions, such as the loss of necrotic chondrocytes and cartilage erosion of more than 200 mg/kg b.w., comparable to or better than a positive drug control (JOINS™,200 mg/kg) in the cartilage of MIA-OA rats.ConclusionsOur results demonstrate that ALM16 has a strong chondroprotective effect against the OA model in vitro and in vivo, likely attributed to its anti-inflammatory activity and inhibition of MMP production.

The dried flowers of Chionanthus retusus were extracted with 80% MeOH, and the concentrate was divided into EtOAc, n-BuOH, and H2O fractions. Repeated SiO2, octadecyl SiO2 (ODS), and Sephadex LH-20 column chromatography of the EtOAc fraction led to the isolation of four flavonols (1&ndash, 4), three flavones (5&ndash, 7), four flavanonols (8&ndash, 11), and one flavanone (12), which were identified based on extensive analysis of various spectroscopic data. Flavonoids 4&ndash, 6 and 8&ndash, 11 were isolated from the flowers of C. retusus for the first time in this study. Flavonoids 1, 2, 5, 6, 8, and 10&ndash, 12 significantly inhibited NO production in RAW 264.7 cells stimulated by lipopolysaccharide (LPS) and glutamate-induced cell toxicity and effectively increased HO-1 protein expression in mouse hippocampal HT22 cells. Flavonoids with significant neuroprotective activity were also found to recover oxidative-stress-induced cell damage by increasing HO-1 protein expression. This article demonstrates that flavonoids from C. retusus flowers have significant potential as therapeutic materials in inflammation and neurodisease.

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.

Bone remodeling and homeostasis are largely the result of the coordinated action of osteoblasts and osteoclasts. Osteoblasts are responsible for bone formation. The differentiation of osteoblasts is regulated by the transcription factors, Runx2 and Osterix. Natural products of plant origin are still a major part of traditional medicinal systems in Korea. The root of Lithospermum erythrorhizon Sieb. et Zucc. (LR), the purple gromwell, is an herbal medicine used for inflammatory and infectious diseases. LR is an anti-inflammatory and exerts anticancer effects by inducing the apoptosis of cancer cells. However, the precise molecular signaling mechanisms of osteoblastogenesis as regards LR and osteoblast transcription are not yet known. In this study, we investigated the effects of ethanol (EtOH) extract of LR (LES) on the osteoblast differentiation of C2C12 myoblasts induced by bone morphogenetic protein 4 (BMP4) and the potential involvement of Runx2 and Osterix in these effects. We found that the LES exhibited an ability to induce osteoblast differentiation. LES increased the expression of the osteoblast marker, alkaline phosphatase (ALP), as well as its activity, as shown by ALP staining and ALP activity assay. LES also increased mineralization, as shown by Alizarin Red S staining. Treatment with LES increased the protein levels (as shown by immunoblotting), as well as the transcriptional activity of Runx2 and Osterix and enhanced osteogenic activity. These results suggest that LES modulates osteoblast differentiation at least in part through Runx2 and Osterix.

In this study, the inhibitory activities of fifty plant extracts on IgE-mediated degranulation in the rat basophilic leukemia cell line (RBL-2H3 cells) were measured; the release of interleukin (IL)-4 and β-hexosaminidase from IgE-sensitized cells treated with the plant extracts was measured; and the effects of the plant extracts on cell viability were tested. The results of the analysis of plant extracts at 20 ㎍/㎖, including the aerial part of Magnolia sieboldii K. Koch, exhibited suppressive activities upon the release of IL-4. Furthermore, several plant extracts including methanol extracted from Lindera erythrocarpa Makino (aerial part) at the same concentration significantly inhibited the release of β-hexosaminidase. Twenty-six of the plant extracts, including methanol extract of Weigela subsessilis (Nakai) L. H. Bailey (branch), showed a cell proliferation effect of over 80% at 100 ㎍/㎖. In conclusion, the results suggest that the leaf/stem of Geum japonicum Thunb. and the stamen/ovary of Nelumbo nucifera Gaertn., which exhibited effective inhibition on β-hexosaminidase release and IL-4 release from mast cells and showed high cell viability, could be useful candidates as anti-allergy materials.

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).

Background : A series of studies were conducted to optimize adventitious root induction in vitro from explants of Astragalus membranaceus using various nutrient media supplemented with plant hormones. Methods and Results : Levels of active components were analyzed from adventitious roots induced under different media conditions. Among the different media conditions, Murashige and Skoog medium supplemented with indole-3-butyric acid resulted in the greatest adventitious root induction rate. The amount of the major active component of the adventitious roots of Ama1, calycosin-7-O--D-glucopyranoside was higher than that of other adventitious root samples. Conclusions : These results suggest that the adventitious roots of A. membranaceus could be used for the commercial production of medicines.

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.

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).

Whistler mode chorus waves are considered to play a central role in accelerating and scattering electrons in the outer radiation belt. While in situ measurements are usually limited to the trajectories of a small number of satellites, rigorous theoretical modeling requires a global distribution of chorus wave characteristics. In the present work, by using a large database of chorus wave observations made on the Time History of Events and Macroscale Interactions during Substorms satellites for about 5 years, we develop prediction models for a global distribution of chorus amplitudes. The development is based on two main components: (a) the temporal dependence of average chorus amplitudes determined by correlating with the preceding solar wind and geomagnetic conditions as represented by the interplanetary magnetic field (IMF) Bz and AE index and (b) the determination of spatial distribution pattern of chorus amplitudes, specifically, the profiles in L in all 2 h magnetic local time zones, which are categorized by activity levels of either the IMF Bz or AE index. Two separate models are developed: one based only on the IMF Bz and the other based only on AE. Both models predict chorus amplitudes for two different latitudinal zones separately: |magnetic latitude (MLAT)

A new neolignan was isolated from the EtOAc fraction obtained from Magnolia obovata fruits. The chemical structure of the new neolignan was determined to be 5,5′-diallyl-2,2′-dihydroxybiphenyl ether (1), named isoobovatol, based on physicochemical and spectroscopic data including FT-NMR and EI-MS.

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.

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.

Background: Cordyceps militaris is one of well-known medicinal mushrooms with anti-inflammatory, anti-cancer, anti-diabetic, and anti-obesity activities. Objective: The objective of the following study is to isolate chemical components from the ethanol extract (Cm-EE) from Cordyceps militaris and to evaluate their anti-inflammatory activities. Materials and Methods: Column chromatographic separation was performed and anti-inflammatory roles of these compounds were also examined by using NO production and protein kinase B (AKT) activity assays. Results: From Cm-EE, 13 constituents, including trehalose (1), cordycepin (2), 6-hydroxyethyladenosine (3), nicotinic amide (4), butyric acid (5), β-dimorphecolic acid (6), α-dimorphecolic acid (7), palmitic acid (8), linoleic acid (9), cordycepeptide A (10), 4-(2-hydroxy-3-((9E,12E)-octadeca-9,12-dienoyloxy)propoxy)-2-(trimethylammonio)butanoate (11), 4-(2-hydroxy-3-(palmitoyloxy)propoxy)-2-(trimethylammonio)butanoate (12), and linoleic acid methyl ester (13) were isolated. Of these components, compound 2 displayed a significant inhibitory effect on NO production in lipopolysaccharide (LPS)-activated RAW264.7 cells. Furthermore, this compound strongly and directly suppressed the kinase activity of AKT, an essential signalling enzyme in LPS-induced NO production, by interacting with its ATP binding site. Conclusion: C. militaris could have anti-inflammatory activity mediated by cordycepin-induced suppression of AKT.

Centella asiatica (L.) Urban contains two ursane-type triterpene saponins, asiaticoside and madecassoside, as major secondary metabolites. In order to select candidate genes encoding UDP-glucosyltransferases (UGTs) involved in asiaticoside biosynthesis, we performed transcriptomic analysis of leaves elicited by methyl jasmonate (MeJA). Among the unigenes, 120 isotigs and 13 singletons of unique sequences were annotated as UGTs, including 37 putative full-length cDNAs, and 15 of the putative UGT genes were named according to the UGT committee nomenclature protocols. One of them, UGT73AH1, was characterized by heterologous expression in Escherichia coli BL21 (DE3) cells. After induction with IPTG, a total protein extract was assayed with UDP-glucose and asiatic acid. UPLC-QTOF/MS analysis showed that UGT73AH1 catalyzes the glycosylation of asiatic acid to its monoglucoside. It remains unclear whether glycosylation occurs on the triterpene C-2α, C-3β, C-23, or C-28 position. However, it is very likely that UGT73AH1 glucosylates the C-28 position, because only C-28 bears a glucose moiety in the final pathway product of asiatic acid, while C-2α, C-3β, and C-23 remain un-conjugated.

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.

The roots of Lythrum salicaria L. were extracted in 80% aqueous MeOH and the concentrated extract was fractionated with EtOAc, n-BuOH, and , successively. The repeated silicagel and octadecyl column chromatographies of the EtOAc fractions led to isolation of an antioxidant compound and two major compounds. From the results of spectral data and the chemical characteristics including nuclear magnetic resonance, MS, and IR, the structures of compounds were determind as myricetin-3-O--D-glucopyranoside (1), oleanolic acid (2), betulinic acid (3). This is the first reported isolation of compounds (1, 2) from L. salicaria. Compound 1 as well as EtOAc, n-BuOH, and solvent fractions were evaluated for 2,2-dipicryl-1-phenylhydrazyl radical scavenging activity.

In this study, the effect of plant extract on the senescence action and cell survival rate in two types of cells, in which aging was derived by adriamycin, was analyzed to find the materials for suppressing cell senescence from natural resources. The results are as follows. For human umbilical vein endothelial cells (HUVECs), the fruit of Physalis angulate L. and the aerial part of Synurus deltoides (Aiton) Nakai showed excellent cell-senescence inhibition activities in a treatment concentration-dependent manner, demonstrating the high possibility for utilization as a material for prevention and treatment for vascular diseases. The water extract from the root of Polygonatum odoratum var. pluriflorum for variegatum Y. N. Lee showed potent cell-senescence inhibitory effect for human dermal fibroblasts (HDFs). Thus it is considered that the additional study on the plant needs for elucidating the possible utilization as material for skin health improvement.

*Department of Herbal Crop Research, NIHHS, RDA, Eumseong 369-873, Korea.**Department of Oriental Pharmacy, College of Pharmacy and Wonkwang-Oriental Medicines Research Institute,Institute of Biotechnology, Wonkwang University, Iksan 570-749, Korea.***BK21 Plus Team, Professional Graduate School of Oriental Medicine, Wonkwang University, Iksan 570-749, Korea.ABSTRACT : Methicillin-resistant Staphylococcus aureus (MRSA) is a substantial contributor to morbidity and mortality.In search of a natural products capable of inhibiting this multidrug resistant bacteria, we have investigated the antimicro-bial activity of brazilein (BRZ) isolated from Caesalpinia sappan L. (Leguminosae) against 8 different strains of Staphylococ-cus aureus (S. aureus). New antimicrobial activity was found using the minimum inhibitory concentrations (MICs), brothdilution as well as checkerboard method. Against the 8 strains, the minimum inhibitory concentrations of BRZ were in therange of 62.5-500㎍/mL. From those results we performed the checkerboard test to determine the synergism of BRZ incombination with Hygromycin-b (HgB) against 4 strains. The combined activity of BRZ and HgB against 4 strains resultedin a fractional inhibitory concentrations index (FICI) ranging from 0.18-0.5. The effect of BRZ with HgB was found to besynergistic. We found that BRZ reduced the MICs of HgB. BRZ and HgB could lead to the development of new combinationantibiotics against MRSA infection. Key Words : Antibacterial Effect, Methicillin-Resistant Staphylococcus aureus, Brazilein, Hygromycin-b

Whistler mode chorus wave is considered to play a critical role in accelerating and precipitating the electrons in the outer radiation belt. In this paper we test a conventional scenario of triggering chorus using THEMIS satellite observations of waves and particles. Specifically, we test if the chorus onset is consistent with development of anisotropy in the electron phase space density (PSD). After analyzing electron PSD for 73 chorus events, we find that, for ~80 % of them, their onsets are indeed associated with development of the positive anisotropy in PSD where the pitch angle distribution of electron velocity peaks at 90 degrees. This PSD anisotropy is prominent mainly at the electron energy range of ≤ ~20 keV. Interestingly, we further find that there is sometimes a time delay among energies in the increases of the anisotropy: A development of the positive anisotropy occurs earlier by several minutes for lower energy than for an adjacent higher energy.