• Title/Summary/Keyword: Organic IC

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Bioassay-Guided Isolation and Identification of Compounds from Arecae Pericarpium with Anti-inflammatory, Anti-oxidative, and Melanogenesis Inhibition Activities

  • Indriana, Amelia;Lee, Kyoung Jin;Kim, Yeong Shik
    • Natural Product Sciences
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    • v.22 no.3
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    • pp.193-200
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    • 2016
  • This study describes the anti-inflammatory, anti-oxidant, and melanogenesis inhibition activities of methanol extract and various organic solvent fractions of Arecae Pericarpium. We examined the inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells, 1,1-diphenyl-2-picrylhydrazine (DPPH) scavenging activity, mushroom tyrosinase inhibition activity and melanin contents. The study showed that, among all tested fractions, methylene chloride fraction showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells ($IC_{50}$ value $8.89{\mu}g/mL$) and DPPH radical scavenging activity ($EC_{50}$ value $21.39{\mu}g/mL$). Methylene chloride and ethyl acetate fractions similarly inhibited mushroom tyrosinase activity. Methanol extract exhibited strongest reduction of melanin content in B16F10 melanoma cells. Based on the bioactivity assay results, methylene chloride and ethyl acetate fractions were further separated. Eight phenolic compounds were isolated, which are dimeric syringol (1), catechol (2), 4-hydroxybenzaldehyde (3), vanillin (4), 4-hydroxyacetophenone (5), apocynin (6), protocatechuic acid (7) and 4-hydroxybenzoic acid (8). Among the isolated compounds tested, catechol showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells. Catechol also showed the concentration-dependent NF-${\kappa}B$ inhibition activity. Arecae Pericarpium might have potentials to be developed as anti-inflammatory agent or dermatological product for skin-whitening agent.

Identification of Alkylation-Sensitive Target Chaperone Proteins and Their Reactivity with Natural Products Containing Michael Acceptor

  • Liu, Xi-Wen;Sok, Dai-Eun
    • Archives of Pharmacal Research
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    • v.26 no.12
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    • pp.1047-1054
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    • 2003
  • Molecular chaperones have a crucial role in the folding of nascent polypeptides in endoplasmic reticulum. Some of them are known to be sensitive to the modification by electrophilic metabolites of organic pro-toxicants. In order to identify chaperone proteins sensitive to alkyators, ER extract was subjected to alkylation by 4-acetamido-4 -maleimidyl-stilbene-2,2 -disulfonate (AMS), and subsequent SDS-PAGE analyses. Protein spots, with molecular mass of 160, 100, 57 and 36 kDa, were found to be sensitive to AMS alkylation, and one abundant chaperon protein was identified to be protein disulfide isomerase (PDI) in comparison with the purified PDI. To see the reactivity of PDI with cysteine alkylators, the reduced form ($PDI_{red}$) of PDI was incubated with various alkylators containing Michael acceptor structure for 30 min at $38^{\circ}C$ at pH 6.3, and the remaining activity was determined by the insulin reduction assay. Iodoacetamide or N-ethylmaleimide at 0.1 mM remarkably inactivated $PDI_{red}$ with N-ethylmaleimide being more potent than iodoacetamide. A partial inactivation of $PDI_{oxid}$ was expressed by iodoacetamide, but not N-ethylmaleimide (NEM) at pH 6.3. Of Michael acceptor compounds tested, 1,4-benzoquinone ($IC_{50}, 15 \mu$ M) was the most potent, followed by 4-hydroxy-2-nonenal and 1,4-naphthoquinone. In contrast, 1,2-naphthoquinone, devoid of a remarkable inactivation action, was effective to cause the oxidative conversion of $PDI_{red}$ to $PDI_{oxid}$. Thus, the action of Michael acceptor compounds differed greatly depending on their structure. Based on these, it is proposed that POI, one of chaperone proteins in ER, could be susceptible to endogenous or xenobiotic Michael acceptor compounds in vivo system.

DEPRESSION: CELLULAR AND PHYSIOLOGICAL CONSEQUENCES OF STRESS (ANTIDEPRESSANT EFFECT OF SEROTONIN N-ACETYLTRANSFERASE INHIBITOR)

  • Kim Kyong-Tai
    • Proceedings of the Korean Society of Food Science and Nutrition Conference
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    • 2001.12a
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    • pp.22-37
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    • 2001
  • Melatonin is secreted during the hours of darkness and is thought to influence the circadian and seasonal timing of a variety of physiological processes. Serotonin N-acetyltransferase (AA-NAT) which is found to be expressed in pineal gland, retina, and various tissues, catalyses the conversion of serotonin to N-acetylserotonin and is known as the rate-limiting enzyme in the biosynthetic pathway of melatonin. The compounds that modulate the activity of AA-NAT can be used to treat serotonin-and melatonin-related diseases such as insomnia, depression and seasonal affective disorders (SAD). Several assay methods have been developed by which to measure AA-NAT activity. We have also developed a simple, rapid and sensitive AA-NAT assay method that takes advantage of differences in the organic solubilities between acetyl CoA and N-acetyltryptamine. We screened modulators of AA-NAT activity from the water extracts of the medicinal plants. We found MNP1005 which strongly inhibited the activity of AA-NAT ($IC_{50}$=2.2$\mu$M). Enzyme inhibitory kinetic studies revealed that MNP1005 exhibited a noncompetitive inhibition toward tryptamine. The antidepressant effect of MNP1005 was investigated on behavioral despair test so called forced swimming test (FST). MNP1005 significantly increased swimming behavior by reducing immobility with treatment of 10 mg/kg when compared to the vehicle-treated control group (P < 0.05). This suggests that MNP1005 possesses antidepressant activity. The influence of chronic MNP1005 treatment on the expression of brain-derived neurotrophic factor (BDNF) was examined by in situ hybridization and Northern blot. Chronic treatment of MNP1005 blocked the downregulation of BDNF mRNA in the frontal cortex and other cortex regions in response to restraint stress.

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Manufacturing of Calcium Binding Peptide using Sericin Hydrolysate and Its Bioavailability in Calcium Deficient Rat (실크 세리신 단백질 가수분해물을 이용한 유기 칼슘제의 제조 및 칼슘 결핍 쥐에서의 생체 이용률)

  • Cho, Hye-Jin;Lee, Hyun-Sun;Jung, Eun-Young;Suh, Hyung-Joo
    • Journal of the East Asian Society of Dietary Life
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    • v.20 no.5
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    • pp.680-686
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    • 2010
  • Silk sericin protein was hydrolyzed by seven proteolytic enzymes in order to examine the effectiveness of the hydrolysates in binding calcium. The amino acid nitrogen content of hydrolysates from Flavourzyme was higher than that for other enzymes, and its calcium binding capacity showed a dose-dependent increase. We examined the effects of calcium binding peptide from sericin hydolysates on the bioavailability of Ca-deficient rats. Three-week-old male rats were fed an Ca-deficient diet for three weeks. Rats were divided into four groups (DD: non-treated group on calcium deficient diet; DD+MC: milk-calcium treated group; DD+OC: organic calcium made using sericin hydolysates; and DD+IC: inorganic calcium ($CaCl_2$). After oral administration of calcium supplements for one week, the calcium content of the serum and liver were significantly higher in DD+OC ($101.7{\mu}g$/mL and $49.3{\mu}g$/mL) and DD+MC ($83.6{\mu}g$/mL and $42.8{\mu}g$/mL) than DD ($86.3{\mu}g$/mL and $43.4{\mu}g$/mL). The alkaline phosphatase (ALP) content in the treated groups was significantly lower than DD, but no significant difference among groups was shown. Aspartate aminotransferase (AST) levels did not show any significant difference between groups. Alanine aminotransferase (ALT) levels were significantly reduced compared to the DD group. In conclusion, binding calcium to peptides from sericin hydrolysates seems to improve its bioavailability, and to hasten the cure of calcium deficiency in experimental rats.

Thermal Behavior of LixCoO2 Cathode and Disruption of Solid Electrolyte Interphase Film

  • Doh, Chil-Hoon;Kim, Dong-Hun;Lee, Jung-Hun;Lee, Duck-Jun;Jin, Bong-Soo;Kim, Hyun-Soo;Moon, Seong-In;Hwang, Young-Gi;Veluchamy, Angathevar
    • Bulletin of the Korean Chemical Society
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    • v.30 no.4
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    • pp.783-786
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    • 2009
  • Thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) and ion chromatography(IC) were employed to analyze the thermal behavior of $Li_xCoO_2$ cathode material of lithium ion battery. The mass loss peaks appearing between 60 and 125 ${^{\circ}C}$ in TGA and the exothermic peaks with 4.9 and 7.0 J/g in DSC around 75 and 85 ${^{\circ}C}$ for the $Li_xCoO_2$ cathodes of 4.20 and 4.35 V cells are explained based on disruption of solid electrolyte interphase (SEI) film. Low temperature induced HF formation through weak interaction between organic electrolyte and LiF is supposed to cause carbonate film disruption reaction, $Li_2CO_3\;+\;2HF{\rightarrow}\;2LiF\;+\;CO_2\;+\;H_2O$. The different spectral DSC/TGA pattern for the cathode of 4.5 V cell has also been explained. Presence of ionic carbonate in the cathode has been identified by ion chromatography and LiF reported by early researchers has been used for explaining the film SEI disruption process. The absence of mass loss peak for the cathode washed with dimethyl carbonate (DMC) implies ionic nature of the film. The thermal behavior above 150 ${^{\circ}C}$ has also been analyzed and presented.

Types & Characteristics of Chemical Substances used in the LCD Panel Manufacturing Process (LCD 제조공정에서 사용되는 화학물질의 종류 및 특성)

  • Park, Seung-Hyun;Park, Hae Dong;Ro, Jiwon
    • Journal of Korean Society of Occupational and Environmental Hygiene
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    • v.29 no.3
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    • pp.310-321
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    • 2019
  • Objectives: The purpose of this study was to investigate types and characteristics of chemical substances used in LCD(Liquid crystal display) panel manufacturing process. Methods: The LCD panel manufacturing process is divided into the fabrication(fab) process and module process. The use of chemical substances by process was investigated at four fab processes and two module processes at two domestic TFT-LCD(Thin film transistor-Liquid crystal display) panel manufacturing sites. Results: LCD panels are manufactured through various unit processes such as sputtering, chemical vapor deposition(CVD), etching, and photolithography, and a range of chemicals are used in each process. Metal target materials including copper, aluminum, and indium tin oxide are used in the sputtering process, and gaseous materials such as phosphine, silane, and chlorine are used in CVD and dry etching processes. Inorganic acids such as hydrofluoric acid, nitric acid and sulfuric acid are used in wet etching process, and photoresist and developer are used in photolithography process. Chemical substances for the alignment of liquid crystal, such as polyimides, liquid crystals, and sealants are used in a liquid crystal process. Adhesives and hardeners for adhesion of driver IC and printed circuit board(PCB) to the LCD panel are used in the module process. Conclusions: LCD panels are produced through dozens of unit processes using various types of chemical substances in clean room facilities. Hazardous substances such as organic solvents, reactive gases, irritants, and toxic substances are used in the manufacturing processes, but periodic workplace monitoring applies only to certain chemical substances by law. Therefore, efforts should be made to minimize worker exposure to chemical substances used in LCD panel manufacturing process.

Anti-Glyaction and Radical Scavenging Activities of Ligustri Fructus by Extraction Method (추출 방법에 따른 여정실의 최종당화산물 생성 저해 및 라디칼 소거 활성)

  • Jeong, Yun Hee;Kim, Seo Yoon;Jeong, Gyeong Han;Kim, Tae Hoon
    • The Korea Journal of Herbology
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    • v.33 no.4
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    • pp.95-100
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    • 2018
  • Objectives : Ligustri Fructus has been used since ancient times as a medicinal usages in folk medicines against antitumor purpose. Many biological active constituents have been identified from this biomass such as several terpenoids and lignans. In current study, the properties of antioxidant and anti-diabetic complications using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)($ABTS^+$) radicals scavenging, and advanced glycation end products (AGEs) inhibition assays were evaluated by different extraction methods of Ligustri Fructus. Methods : In present continuing research for development of bioactive natural ingredients, antioxidant and AGEs formation inhibitory capacities of Ligustri Fructus extracts using different organic solvents were prepared and the biological potentials were investigated using in vitro bioassays. Antioxidant properties were evaluated employing radical scavenging assays using DPPH and $ABTS^+$ radicals. In addition, the anti-diabetic complications effects of Ligustri Fructus extracts were tested via AGEs formation inhibitory assay. The total phenolic contents were determined using a spectrophotometric method. Results : All the tested extracts exhibited dose-dependent radical scavenging and AGEs formation inhibitory activities. Among the tested samples, hot water extract of Ligustri Fructus was showed the most potent activity with $IC_{50}$ value of $494.8{\pm}6.7{\mu}g/m{\ell}$ against DPPH radical scavenging assay. Also, $ABTS^+$ radical scavenging activity of hot water extract was higher than those of other extracts. In addition, AGEs formation inhibitory effects of each extacts and total phenolic contents were evaluated. Conclusions : These results suggested that Ligustri Fructus can be considered as a new effective source of natural antioxidant and anti-diabetic complications resources.

Synthesis of Novel Kojic Acid Derivative and Its Anti-pigmentation Effect

  • Kim, K. H.;Kim, K. S.;Kim, J. G.;Park, S. H.;E. K. Yang;Park, S. N.
    • Proceedings of the SCSK Conference
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    • 2003.09a
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    • pp.719-732
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    • 2003
  • A kojic acid derivative, kojic acid 7-O-$\beta$-D-tetraacetylglucopyranoside(KTG) was synthesized. Regio-and stereo-selective glycosylation at 7-postion in kojic acid with $\beta$-D-pentaacetylglucose was achieved with high yield(80%) by the use of Lewis acid and organic base in nonpolar solvent. KTG was hydrolyzed in methanol by the aid of sodium methoxide to give kojic acid 7-O-$\beta$-D-glucopyranoside(KGP). KGP is freely soluble in water and soluble in methanol and ethanol. Its structure was comfirmed by $^1$H-NMR and $^{13}$ C-NMR. Tyrosinase activity inhibition of KGP was measured with mushroom tyrosinase compared with ascorbic acid, kojic acid and arbutin. KGP showed higher tyrosinase inhibition activity($IC_{50}$/=33.3 $\mu\textrm{g}$/ml) than ascorbic acid(63.2 $\mu\textrm{g}$/ml) and arbutin(91.8 $\mu\textrm{g}$/ml) but lower inhibition activity than kojic acid(8.3 $\mu\textrm{g}$/ml). To test free-radical scavenging activity, we used 1, 1-diphenyl-2-picrylhydrazyl(DPPH) as a free-radical source. Free-radical scavenging activity of KGP was very low($SC_{50}$/>1000 $\mu\textrm{g}$/ml) compared with ascorbic acid($SC_{50}$/=2.68 $\mu\textrm{g}$/ml) and arbutin($SC_{50}$/=180$\mu\textrm{g}$/ml). Melanin formation inhibition of KGP was measured in B16 melanoma, compared with kojic acid, arbutin and Vitamin C. Inhibition activity of KGP for melanin formation was not found within test concentrations.

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Gene Expression Profiles and Antioxidant Effects of Houttuynia cordata Thunb Extract in Human Keratinocyte HaCaT Cells (인간 피부각질세포 HaCaT에서 어성초 추출물의 유전체 발현 분석 및 항산화 효과)

  • Kim, Jung Min;Bang, In Seok
    • Journal of Life Science
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    • v.28 no.12
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    • pp.1406-1415
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    • 2018
  • Based on the antioxidative effects in organic solvent fractions obtained from the main methanolic extract of Houttuynia cordata Thunb, the cytoprotective effects by oxidative-stress were here analyzed. Regarding the antioxidant activity of organic solvent fractions, the electron-donating ability of DPPH increased in a dose-dependent manner, and $ED_{50}$ exhibited the highest concentration at $175{\mu}g/ml$ in the Hc-EtOAc fraction. The cell viability of Hc-EtOAc fractions on $H_2O_2$-induced HaCaT cell death ($IC_{50}$) increased in a concentration-dependent manner and a visible cell survival rate of 74% was observed at a concentration of $100{\mu}g/ml$. Meanwhile, the gene expression patterns in HaCaT cells treated with $100{\mu}g/ml$ of the Hc-EtOAc fraction for 6 and 24 hr were identified with microarray analysis. The genes involved in signal transduction, cell division, antioxidant activity, and epithelial cell proliferation were found to be 2-fold up-regulated genes in HaCaT cells following the Hc-EtOAc fraction treatment. Especially, proinflammatory cytokines (IL1B, TNF, and IL6) were identified as involved in antioxidant activity based on the expression patterns of the HaCaT cells, and pathway analysis indicated that TLR4 might be considered an upstream regulator of these genes. In order to verify the activity of IL1B, TNF, and IL6, qRT-PCR showed that the expression increased more than 2 times in HaCaT cells treated with at least $100{\mu}g/ml$ of the Hc-EtOAc fraction. The activity of the upstream regulator TLR4 protein was also increased by the Hc-EtOAc fraction. As a result, the antioxidative activity of the Hc-EtOAc fraction is predicted to pass from TLR4 through cytokines such as IL1B, TNF, and IL6.

Applicability evaluation of GIS-based erosion models for post-fire small watershed in the wildland-urban interface (WUI 산불 소유역에 대한 GIS 기반 침식모형의 적용성 평가)

  • Shin, Seung Sook;Ahn, Seunghyo;Song, Jinuk;Chae, Guk Seok;Park, Sang Deog
    • Journal of Korea Water Resources Association
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    • v.57 no.6
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    • pp.421-435
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    • 2024
  • In April 2023, a wildfire broke out in Gangneung located in the east coast region due to the influence of the Yanggang-local wind. In this study, GIS-based RUSLE(Revised Universal Soil Loss Equation) and SEMMA (Soil Erosion Model for Mountain Areas) were used to evaluate the erosion rate due to vegetation recovery in a small watershed of the Gangneung WUI(Wildland-Urban Interface) fire. The small watershed of WUI fire has a low altitude range of 10-30 m and the average slope of 10.0±7.4° which corresponds to a gentle slope. The soil texture was loamy sand with a high organic content and the deep soil depth. As herbaceous layer regenerated profusely in the gully after the wildfire, the NDVI (Normalized Difference Vegetation Index) reached a maximum of 0.55. Simulation results of erosion rates showed that RUSLE ranged from 0.07-94.9 t/ha/storm and SEMMA ranged from 0.24-83.6 t/ha/storm. RUSLE overestimated the average erosion rate by 1.19-1.48 times compared to SEMMA. The erosion rates were estimated to be high in the middle slope where burned pine trees were widely distributed and the slope was steep and to be relatively low in the hollow below the gully where herbaceous layer recovers rapidly. SEMMA showed a rapid increase in erosion sensitivity under at certain vegetation covers with NDVI below 0.25 (Ic = 0.35) on post-fire hillslopes. Gentle slopes with high organic content and rapid recovery of natural vegetation had relatively low erosion rate compared to steep slopes. As subsequent infrastructure and human damages due to sediment disaster by heavy rain is anticipated in WUI fire areas, the research results may be used as basic data for targeted management and decision making on the implementation of emergency treatment after the wildfire.