• Title/Summary/Keyword: leading compound

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Suppression of Inflammatory Responses by Black Rice Extract in RAW 264.7 Macrophage Cells via Downregulation of NF-kB and AP-1 Signaling Pathways

  • Limtrakul, Pornngarm;Yodkeeree, Supachai;Pitchakarn, Pornsiri;Punfa, Wanisa
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.10
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    • pp.4277-4283
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    • 2015
  • Anthocyanin, a phenolic compound, has been reported to have an anti-inflammatory effect against lipopolysaccharide (LPS) induced changes in immune cells. However, little is known about the molecular mechanisms underlying its anti-inflammatory effects. Few research studies have concerned the anti-inflammation properties of colored rice extract as a functional material. Therefore, the purpose of this study was to examine anti-inflammatory effects of the polar fraction of black rice whole grain extracts (BR-WG-P) that features a high anthocyanin content. Our results showed that BR-WG-P significantly inhibited LPS-induced pro-inflammatory mediators, including production of NO and expression of iNOS and COX-2. In addition, secretion of pro-inflammatory cytokines including TNF-${\alpha}$ and IL-6 was also significantly inhibited. Moreover, BR-WG-P and anthocyanin inhibited NF-kB and AP-1 translocation into the nucleus. BR-WG-P also decreased the phosphorylation of ERK, p38 and JNK in a dose dependent manner. These results suggested that BR-WG-P might suppress LPS-induced inflammation via the inhibition of the MAPK signaling pathway leading to decrease of NF-kB and AP-1 translocation. All of these results indicate that BR-WG-P exhibits therapeutic potential associated with the anthocyanin content in the extract for treating inflammatory diseases associated with cancer.

Phospholipase Activities in Clinical and Environmental Isolates of Acanthamoeba

  • Matin, Abdul;Jung, Suk-Yul
    • Parasites, Hosts and Diseases
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    • v.49 no.1
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    • pp.1-8
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    • 2011
  • The pathogenesis and pathophysiology of Acanthamoeba infections remain incompletely understood. Phospholipases are known to cleave phospholipids, suggesting their possible involvement in the host cell plasma membrane disruption leading to host cell penetration and lysis. The aims of the present study were to determine phospholipase activities in Acanthamoeba and to determine their roles in the pathogenesis of Acanthamoeba. Using an encephalitis isolate (T1 genotype), a keratitis isolate (T4 genotype), and an environmental isolate (T7 genotype), we demonstrated that Acanthamoeba exhibited phospholipase $A_2$ (PLA$_2$). and phospholipase D (PLD) activities in a spectrophotometry-based assay. Interestingly, the encephalitis isolates of Acanthamoeba exhibited higher phospholipase activities as compared with the keratitis isolates, but the environmental isolates exhibited the highest phospholipase activities. Moreover, Acanthamoeba isolates exhibited higher PLD activities compared with the PLA$_2$. Acanthamoeba exhibited optimal phospholipase activities at $37^{\circ}C$ and at neutral pH indicating their physiological relevance. The functional role of phospholipases was determined by in vitro assays using human brain microvascular endothelial cells (HBMEC), which constitute the blood-brain barrier. We observed that a PLD-specific inhibitor, i.e., compound 48/80, partially inhibited Acanthamoeba encephalitis isolate cytotoxicity of the host cells, while PLA$_2$-specific inhibitor, i.e., cytidine 5'-diphosphocholine, had no effect on parasite-mediated HBMEC cytotoxicity. Overall, the T7 exhibited higher phospholipase activities as compared to the T4. In contract, the T7 exhibited minimal binding to, or cytotoxicity of, HBMEC.

The Materials Science of Chalcopyrite Materials for Solar Cell Applications

  • Rockett, Angus
    • Proceedings of the Korean Vacuum Society Conference
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    • 2011.08a
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    • pp.53-53
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    • 2011
  • This paper describes results for surface and bulk characterization of the most promising thin film solar cell material for high performance devices, (Ag,Cu) (In,Ga) Se2 (ACIGS). This material in particular exhibits a range of exotic behaviors. The surface and general materials science of the material also has direct implications for the operation of solar cells based upon it. Some of the techniques and results described will include scanning probe (AFM, STM, KPFM) measurements of epitaxial films of different surface orientations, photoelectron spectroscopy and inverse photoemission, Auger electron spectroscopy, and more. Bulk measurements are included as support for the surface measurements such as cathodoluminescence imaging around grain boundaries and showing surface recombination effects, and transmission electron microscopy to verify the surface growth behaviors to be equilibrium rather than kinetic phenomena. The results show that the polar close packed surface of CIGS is the lowest energy surface by far. This surface is expected to be reconstructed to eliminate the surface charge. However, the AgInSe2 compound has yielded excellent atomic-resolution images of the surface with no evidence of surface reconstruction. Similar imaging of CuInSe2 has proven more difficult and no atomic resolution images have been obtained, although current imaging tunneling spectroscopy images show electronic structure variations on the atomic scale. A discussion of the reasons why this may be the case is given. The surface composition and grain boundary compositions match the bulk chemistry exactly in as-grow films. However, the deposition of the heterojunction forming the device alters this chemistry, leading to a strongly n-type surface. This also directly explains unpinning of the Fermi level and the operation of the resulting devices when heterojunctions are formed with the CIGS. These results are linked to device performance through simulation of the characteristic operating behaviors of the cells using models developed in my laboratory.

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Vasodilator-stimulated phosphoprotein-phosphorylation by ginsenoside Ro inhibits fibrinogen binding to αIIb/β3 in thrombin-induced human platelets

  • Shin, Jung-Hae;Kwon, Hyuk-Woo;Cho, Hyun-Jeong;Rhee, Man Hee;Park, Hwa-Jin
    • Journal of Ginseng Research
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    • v.40 no.4
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    • pp.359-365
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    • 2016
  • Background: Glycoprotein IIb/IIIa (${\alpha}aIIb/{\beta}_3$) is involved in platelet adhesion, and triggers a series of intracellular signaling cascades, leading to platelet shape change, granule secretion, and clot retraction. In this study, we evaluated the effect of ginsenoside Ro (G-Ro) on the binding of fibrinogen to ${\alpha}aIIb/{\beta}_3$. Methods: We investigated the effect of G-Ro on regulation of signaling molecules affecting the binding of fibrinogen to ${\alpha}aIIb/{\beta}_3$, and its final reaction, clot retraction. Results: We found that G-Ro dose-dependently inhibited thrombin-induced platelet aggregation and attenuated the binding of fibrinogen to ${\alpha}aIIb/{\beta}_3$ by phosphorylating cyclic adenosine monophosphate (cAMP)-dependently vasodilator-stimulated phosphoprotein (VASP; $Ser^{157}$). In addition, G-Ro strongly abrogated the clot retraction reflecting the intensification of thrombus. Conclusion: We demonstrate that G-Ro is a beneficial novel compound inhibiting ${\alpha}aIIb/{\beta}_3$-mediated fibrinogen binding, and may prevent platelet aggregation-mediated thrombotic disease.

Exploration of the Glycosyltransferase BmmGT1 from a Marine-Derived Bacillus Strain as a Potential Enzyme Tool for Compound Glycol-Diversification

  • Liu, Quanquan;Ren, Pengfei;Liu, Yang;Qin, Wen;Li, Huayue;Li, Wenli
    • Journal of Microbiology and Biotechnology
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    • v.28 no.6
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    • pp.931-937
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    • 2018
  • Glycosyltransferases (GTs) from microbes are an emerging and rich source for efficient glycol-transformation of natural/unnatural compounds. Here, we probed the catalytic capability and substrate promiscuity of BmmGT1 from marine-derived Bacillus methylotrophicus B-9987. The regioselectivity of BmmGT1 on macrolactin A (1) was explored by optimization of the reaction conditions, in which a series of O-glycosylated macrolactins (1a-1e) were generated, including two new di/tri-O-glucosyl analogs (1b and 1e). Furthermore, BmmGT1 was able to catalyze the glycosylation of the thiol (S-) or amine (N-) sites of phenolic compounds (2 and 3), leading to the generation of N- (2a) or S-glycosides (3a and 3b). The present study demonstrates that BmmGT1 could serve as a potential enzyme tool for O-, N-, or S-glycosyl structural diversification of compounds for drug discovery.

Zerumbone Restores Gut Microbiota Composition in ETBF Colonized AOM/DSS Mice

  • Cho, Hye-Won;Rhee, Ki-Jong;Eom, Yong-Bin
    • Journal of Microbiology and Biotechnology
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    • v.30 no.11
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    • pp.1640-1650
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    • 2020
  • Colorectal cancer (CRC) is the leading cause of common malignant neoplasm worldwide. Many studies have analyzed compositions of gut microbiota associated with various diseases such as inflammatory bowel diseases (IBD) and colon cancer. One of the most representative bacteria involved in CRC is enterotoxigenic Bacteroides fragilis (ETBF), a species belonging to phylum Bacteroidetes. We used ETBF colonized mice with azoxymethane (AOM)/dextran sulphate sodium (DSS) and zerumbone, a compound with anti-bacterial effect, to determine whether zerumbone could restore intestinal microbiota composition. Four experimental groups of mice were used: sham, ETBF colonized AOM/DSS group, ETBF colonized AOM/DSS group zerumbone 60 mg kg-1 (ETBF/AOM/DSS + Z (60)), and only zerumbone (60 mg kg-1)-treated group. We performed reversible dye terminators-based analysis of 16S rRNA gene region V3-V4 for group comparison. Microbiota compositions of ETBF/AOM/DSS + Z (60) group and ETBF colonized AOM/DSS group not given zerumbone were significantly different. There were more Bacteroides in ETBF/AOM/DSS + Z (60) group than those in ETBF colonized AOM/DSS group, suggesting that B. fragilis could be a normal flora activated by zerumbone. In addition, based on linear discriminant analysis of effect size (LEfSe) analysis, microbial diversity decreased significantly in the ETBF colonized AOM/DSS group. However, after given zerumbone, the taxonomic relative abundance was increased. These findings suggest that zerumbone not only influenced the microbial diversity and richness, but also could be helpful for enhancing the balance of gut microbial composition. In this work, we demonstrate that zerumbone could restore the composition of intestinal microbiota.

Electronic Structure and Chemical Bonding of La7Os4C9 (La7Os4C9의 전자구조와 화학결합)

  • Kang, Dae-Bok
    • Journal of the Korean Chemical Society
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    • v.53 no.3
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    • pp.266-271
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    • 2009
  • In the recently synthesized rare earth transition metal carbide $La_7O_{s4}C_9$ one finds one-dimensional organometallic $[O_{s4}C_9]^{21-}$ polymers embedded in a $La^{3+}$ ionic matrix. The electronic structure of the polymeric $[O_{s4}C_9]^{21-}$ chain was investigated by density of states (DOS) and crystal orbital overlap population (COOP), using the extended Huckel algorithm. A fragment molecular orbital analysis is used to study the bonding characteristics of the $C_2$ units in $La_7O_{s4}C_9$ containing $C_2$ units and single C atoms as well. The title compound contains partially filled Os and carbon bands leading to metallic conductivity. As the observed distances already indicated, the calculations show extensive Os-C interactions. The C-C bond distance in the diatomic $C_2$ units ($d_{C-C}$=131 pm) in the solid is significantly increased relative to $${C_2}^{2-}$$ or acetylene, because antibonding $1{\pi}_g$ orbitals are partially filled by the Os-$C_2(1\;{\pi}_g)$ bonding contribution found at and below the Fermi level.

Nasal Absorption of Procyclidine in Rats and Dogs

  • Jang, Eun-Ju;Lee, Young-Joo;Chung, Suk-Jae;Shim, Chang-Koo
    • Archives of Pharmacal Research
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    • v.24 no.3
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    • pp.219-223
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    • 2001
  • Nasal absorption of procyclidine, a synthetic anticholinergic compound, was investigated in Wistar rats and Beagle dogs. The dosing solution was prepared by dissolving$^{14}C$-procyclidme in 50% ethanolic saline. The dosing solution was administered intravenously and intranasally to rats at a dose of 0.6 mg/kg (i.e., $60{\mu}$l/kg in the form of a 1% w/v solution), and intravenously, orally and intranasally to doss at a dose of 0.3 mg/kg(i.e., $6{mu}$l/kg in the form of a 5% w/v solution). Blood samples were taken from an artery of the animals through the catheter for periods of 1200 (for rats) and 1440 min (for dogs), and the radioactivity in the samples was determined by liquid scintillation counting. The nasal bioavailability of Procyclidine in rats and dogs, based on the radioactivity was calculated to be 81.1 and 98.6% respectively. In both rats and dogs, the plasma profiles of procyclidine following nasal administration were very close to those following intravenous administration, leading to nearly superimposable profiles between the two protocols. In dogs, nasal administration resulted in significantly higher plasma concentrations during the first 30 min period compared to oral administration, suggesting the superiority of the nasal route over the oral route in terms of a prompt expression of the pharmacological effect of the drug. The results obtained in this study indicate that procyclidine is rapidly and nearly completely absorbed via the nasal route. In conclusion, nasal administration represents a viable alternative to intravenous administration in the case of procyclidine.

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Influence of Extrusion on Dietary Fiber Profile and Bioactive Compound in Different Parts of Tatary Buckwheat (Fagopyrum tataricum) (쓴메밀의 서로 다른 부위에서 압출성형이 식이섬유 및 생리활성물질의 함량에 미치는 영향)

  • Kim, Dong-Eun;Hong, Soon-Yeol;Kang, Wie-Soo;Yu, Chang-Yeon;Lee, Beom-Goo;Chung, Ill-Min;Lim, Jung-Dae
    • Korean Journal of Medicinal Crop Science
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    • v.17 no.6
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    • pp.379-387
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    • 2009
  • The aim of this investigation was to examine the influence of extrusion on dietary fiber profile and the content of bioactive compounds, rutin and quercetin in young sprout, whole seed, and matured stem of Tartary buckwheat. WSI(water soluble index) is increased by a function of both screw profile and process temperature, compared to control in different parts of Buckwheat. Also, WSI of ME is increased more than 5.2 times in grain, compared to that of control. The effect of precooking by extrusion on the dietary fiber profile of buckwheat flour was evaluated. Precooking by extrusion significantly increased SDF in flour, although in most cases extrusion decrease in TDF a little. The thermo-mechanical treatment undergone by the buckwheat flour during extrusion led to redistribute part IDF fraction to SDF, leading to an increase in the latter. The content of rutin was increased about two fold in extruded flour of sprout, compared to in control. This increase maybe why these compounds are released from cell wall by high shear processing under high temperature.

Interrelationship between Paleovegetation in Southern and Central California and Northeast Pacific Atmospheric and Oceanographic Processes over the Last ~30 kyr (과거 3만년 동안 캘리포니아 남부와 중부지역의 고식생 변화와 북동태평양 대기 및 해양순환 변동과의 연관성 연구)

  • Suh, Yeon Jee
    • Ocean and Polar Research
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    • v.41 no.3
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    • pp.159-168
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    • 2019
  • Understanding the interaction between climate and the water cycle is critical especially in a drought sensitive region such as California. This study explored hydrologic changes in central and southern California in relation to the glacial-interglacial climate cycles over the last 30 thousand years. To do this, we reconstructed paleovegetation using plant wax carbon isotopic compositions (${\delta}^{13}C$) preserved in marine sediment cores retrieved from the central California continental shelf (ODP Site 1018) and Santa Barbara Basin (ODP Site 893A). The results were then compared to the existing sea surface temperature (SST) and pollen records from the same cores to understand terrestrial hydrology in relation to oceanographic processes. The Last Glacial was generally dry both in central and southern California, indicated by grassland expansion, confirming the previously suggested notion that the westerly storm track that supplies the majority of the precipitation in California may not have moved southward during the glacial period. Southern California was drier than central California during the Last Glacial Maximum (LGM). This drying trend may have been associated with the weakening of the California Current and northerly winds leading to the early increase in SST in southern California and decline in both offshore and coastal upwelling. The climate was wetter during the Holocene in both regions compared to the glacial period and forest coverage increased accordingly. We attribute this wetter condition to the precipitation contribution increase from the tropics. Overall, we found a clear synchronicity between the terrestrial and marine environment which showed that the terrestrial vegetation composition in California is greatly affected by not only the global climate states but also regional oceanographic and atmospheric conditions that regulate the timing and amount of precipitation over California.